Tyrosine Kinase/Adaptors
A tyrosine kinase is an enzyme that can transfer a phosphate group from ATP to a protein in a cell. It functions as an "on" or "off" switch in many cellular functions. Tyrosine kinases are a subclass of protein kinase. The phosphate group is attached to the amino acid tyrosine on the protein. Tyrosine kinases are a subgroup of the larger class of protein kinases that attach phosphate groups to other amino acids (serine and threonine). Phosphorylation of proteins by kinases is an important mechanism in communicating signals within a cell (signal transduction) and regulating cellular activity, such as cell division. Protein kinases can become mutated, stuck in the "on" position, and cause unregulated growth of the cell, which is a necessary step for the development of cancer. Therefore, kinase inhibitors, such as imatinib, are often effective cancer treatments.
Products for Tyrosine Kinase/Adaptors
- FLT3(9)
- c-MET(24)
- Glycogen Synthase Kinase 3(9)
- IRAK(6)
- VEGFR(42)
- c-RET(7)
- Spleen Tyrosine Kinase (Syk)(8)
- CSF-1R(3)
- ALK(14)
- Trk(9)
- FGFR(12)
- Axl(4)
- Src(27)
- PDGFR(17)
- FAK(5)
- IGF1R(7)
- Broad Spectrum Protein Kinase Inhibitor(5)
- HER2(7)
- Insulin Receptor(5)
- EGFR(65)
- EphB4(1)
- LRRK2(9)
- ROR(2)
- Ack1(2)
- Bcr-Abl(4)
- BMX Kinase(1)
- DDR1/DDR2 Receptor(1)
- PTKs/RTKs(3)
- c-Kit(4)
- ITK(2)
- c-FMS(3)
- Pyk2(2)
- Lck(1)
- Tie-2(2)
- Cat.No. Product Name Information
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BCC3661
Nintedanib (BIBF 1120)
Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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BCC1572
Fenretinide
Synthetic retinoid; antiproliferative and antioxidant,Tretinoin, which is a ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR), can induce granulocytic differentiation and apoptosis in acute promyelocytic leukemia (APL) cells.
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BCC1242
AG-1024
AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of insulin receptor (IR; IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
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BCC1243
SU11274
SU11274 is a selective Met inhibitor with IC50 of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.
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BCC6076
BIO-acetoxime
BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.
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BCC3671
Crenolanib (CP-868596)
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
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BCC3964
ZM 306416
ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.
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BCC1948
Silvestrol
Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata. Silvestrol induces autophagy and caspase-mediated apoptosis.
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BCC7132
Herbimycin A
Antiangiogenic. Inhibits Src family kinases and Hsp90
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BCC3971
PF-431396
PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.
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BCC3674
PF-562271
PF-562271 is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.
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BCC1253
OSI-930
OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.
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BCC1406
BAY 61-3606
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
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BCC3646
Regorafenib
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
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BCC1339
ALK inhibitor 1
ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
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BCC3885
TAE226 (NVP-TAE226)
NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively.
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BCC1340
ALK inhibitor 2
ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.
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BCC3660
TAE684 (NVP-TAE684)
NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.
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BCC7189
Demethylasterriquinone B1
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BCC1260
Masitinib (AB1010)
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.
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BCC7356
BIBU 1361 dihydrochloride
Selective inhibitor of EGFR-kinase
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BCC1261
Linifanib (ABT-869)
Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib (ABT-869) shows prominent antitumor activity. Linifanib (ABT-869) has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases.
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BCC6956
RR-src
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BCC5099
Apatinib
Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the treatment of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ.
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BCC2172
Danusertib (PHA-739358)
Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
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BCC1883
Regorafenib hydrochloride
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
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BCC8051
WH-4-023
WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
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BCC6529
GNF-7
GNF-7 inhibits Bcr-Abl WT and Bcr-Abl T315I with IC50 of 133 nM and 61 nM, respectively.
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BCC2553
R406 (free base)
R406 free base is a potent Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3.
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BCC3876
R406
R406 is a competitive Syk inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value.
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BCC1689
Lck Inhibitor
Lck Inhibitor is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM.
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BCC6046
HKI 357
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
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BCC1263
Foretinib (GSK1363089)
Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
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BCC1264
Cabozantinib (XL184, BMS-907351)
Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
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BCC1973
SU14813 maleate
SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
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BCC1330
Afatinib dimaleate
Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
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BCC2258
Amuvatinib (MP-470, HPK 56)
Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
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BCC3771
Dovitinib Dilactic acid
Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
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BCC1517
Dasatinib hydrochloride
Dasatinib hydrochloride (BMS-354825 hydrochloride) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor, with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride has potent antitumor activity.
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BCC2477
Motesanib Diphosphate (AMG-706)
Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
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BCC6104
5'-Fluoroindirubinoxime
5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
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BCC1644
Imatinib hydrochloride
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BCC3697
Linsitinib
Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively.
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BCC1995
TG 100572 Hydrochloride
TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
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BCC1996
TG 100801
TG 100801 is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
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BCC1994
TG 100572
TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
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BCC4496
PF-573228
PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.
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BCC1323
A-770041
A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.
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BCC1096
GW2580
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
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BCC3860
TAK-285
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
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BCC1278
BGJ398
Infigratinib (BGJ-398; NVP-BGJ398) is a potent inhibitor of the FGFR family with IC50s of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
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BCC1333
AIM-100
AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of 24 nM
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BCC6370
PLX647
PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively.
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BCC1426
BMS-599626 Hydrochloride
BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
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BCC2006
Toceranib phosphate
Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
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BCC2479
MGCD-265
MGCD-265-analog (structurally related to MGCD-265) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively.
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BCC1284
(R)-Crizotinib
Crizotinib (PF-02341066) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib (PF-02341066) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib (PF-02341066) is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib (PF-02341066) has effective tumor growth inhibition.
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BCC7441
HDS 029
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BCC6388
AZD2932
AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.
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BCC6078
(E)-FeCP-oxindole
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BCC1472
c-FMS inhibitor
c-Fms-IN-3 is a novel c-Fms kinase inhibitor with a potential as anti-inflammatory agent and antirheumatic agent.
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BCC3970
Flumatinib mesylate
Flumatinib mesylate (HH-GV-678 mesylate), a derivative of imatinib, is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively.
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BCC5080
KX2-391
Tirbanibulin (KX2-391) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
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BCC5082
Fostamatinib (R788)
Fostamatinib (R788), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.
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BCC3688
Tivantinib (ARQ 197)
Tivantinib is a highly selective c-Met tyrosine kinase inhibitor with a Ki of 355 nM.
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BCC3721
AMG-458
AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells.
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BCC6473
Dovitinib (TKI258) Lactate
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BCC3816
MK-2461
MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.
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BCC3677
RAF265
RAF265 is a potent RAF/VEGFR2 inhibitor.
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BCC4423
Golvatinib (E7050)
Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
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BCC1655
IRAK inhibitor 2
IRAK inhibitor 2 is interleukin-1 receptor associated kinase inhibitor .
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BCC2198
TG101209
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
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BCC3684
PF-00562271
PF-562271 besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.
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BCC5587
ACTB-1003
EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2.
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BCC3963
NVP-BHG712
NVP-BHG712 is an oral active EphB4 kinase autophosphorylation inhibitor, with IC50 values of 3.3 nM and 3.0 nM for EphA2 and EphB4, respectively.
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BCC2485
JNJ-38877605
JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
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BCC7662
JNJ 28871063 hydrochloride
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BCC1690
Lck inhibitor 2
Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively
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BCC2561
Tie2 kinase inhibitor
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
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BCC2548
Quizartinib (AC220)
Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
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BCC5583
BLZ945
BLZ945 is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
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BCC2486
PF-04217903
PF-04217903 is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties.
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BCC1849
PF-04217903 methanesulfonate
PF-04217903 methanesulfonate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 methanesulfonate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties.
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BCC7152
K 252a
K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.