XL019JAK2 inhibitor,potent and selective CAS# 945755-56-6 |
- CYT387 sulfate salt
Catalog No.:BCC1506
CAS No.:1056636-06-6
- Baricitinib phosphate
Catalog No.:BCC1401
CAS No.:1187595-84-1
- JAK2 Inhibitor V, Z3
Catalog No.:BCC1667
CAS No.:195371-52-9
- Bardoxolone methyl
Catalog No.:BCC1400
CAS No.:218600-53-4
- Ruxolitinib (INCB018424)
Catalog No.:BCC1276
CAS No.:941678-49-5
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 945755-56-6 | SDF | Download SDF |
PubChem ID | 57990869 | Appearance | Powder |
Formula | C25H28N6O2 | M.Wt | 444.53 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : 25 mg/mL (56.24 mM; Need ultrasonic) | ||
Chemical Name | (2S)-N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide | ||
SMILES | C1CC(NC1)C(=O)NC2=CC=C(C=C2)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCOCC5 | ||
Standard InChIKey | ISOCDPQFIXDIMS-QHCPKHFHSA-N | ||
Standard InChI | InChI=1S/C25H28N6O2/c32-24(23-2-1-12-26-23)28-19-5-3-18(4-6-19)22-11-13-27-25(30-22)29-20-7-9-21(10-8-20)31-14-16-33-17-15-31/h3-11,13,23,26H,1-2,12,14-17H2,(H,28,32)(H,27,29,30)/t23-/m0/s1 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | XL019 is a potent and selective inhibitor of JAK2 with IC50 value of 2.2 nM. | |||||
Targets | JAK2 | |||||
IC50 | 2.2 nM |
XL019 Dilution Calculator
XL019 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.2496 mL | 11.2478 mL | 22.4957 mL | 44.9913 mL | 56.2392 mL |
5 mM | 0.4499 mL | 2.2496 mL | 4.4991 mL | 8.9983 mL | 11.2478 mL |
10 mM | 0.225 mL | 1.1248 mL | 2.2496 mL | 4.4991 mL | 5.6239 mL |
50 mM | 0.045 mL | 0.225 mL | 0.4499 mL | 0.8998 mL | 1.1248 mL |
100 mM | 0.0225 mL | 0.1125 mL | 0.225 mL | 0.4499 mL | 0.5624 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
XL019 is a potent and selective inhibitor of JAK2 with IC50 value of 2.2 nM.
JAK kinases were first identified in 1989 and characterized by the presence of two tyrosine kinase domains. There are four members in the JAK family, which are JAK1, JAK2, JAK3 and TYK2. JAK2 played an important role in the pathways that control erythroid, myeloid and megakaryocytic development. JAK2 mediates signaling through erythropoietin receptor, thrombopoietin receptor and cytokine receptor that harbor the common β-chain (e.g. IL3 receptor) and IFN-γ receptors [38]. JAK2 inhibitors are a novel class of agents with promising results for treating patients with polycythemia vera (PV), essential thrombocythemia (ET) and myelofibrosis (MF) [1]. XL019 was selected as a clinical candidate and advanced into human clinical trials where it was evaluated in patients with PMF, post-PV, or post-ET MF [2].
XL019 shows good biochemical and cellular potency against JAK2 with good selectivity, against a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family [2]. Analogue XL019 was evaluated against a select panel of 118 kinases. Targets for which XL019 exhibited IC50 <1000 nM are displayed. XL019 is a highly selective JAK2 inhibitor displaying >50-fold selectivity against all kinases tested including JAK1 and TYK2. XL019 was a desirable CYP, hERG (16 μM), and P-glycoprotein inhibition (>20 μM).
XL019 had a superior pharmacodynamic profile and thus was evaluated in an efficacy experiment measuring growth inhibition of HEL.92.1.7 xenograft tumors in mice. Derivative XL019 demonstrated 60% and 70% inhibition when dosed orally at 200 mg/kg and 300 mg/kg respectively twice a day for 14 days. Thirty patients received XL019 for a median of 91 days. All of them have discontinued XL019 therapy. Toxicity: N/A Clinical trial: A Safety Study of XL-019 in Adults With Myelofibrosis [2].
References:
[1]. Fabio P.S. Santos, Srdan Verstovsek. JAK2 inhibitors: What's the true therapeutic potential?. Blood Reviews, 2011, 25: 53-63.
[2]. Srdan Verstovsek, Constantine S. Tam, Martha Wadleigh, et al. Phase I evaluation of XL019, an oral, potent, and selective JAK2 inhibitor. Leukemia Research, 2014, 38: 316-322.
- 7-O-ethyl-morroniside
Catalog No.:BCN3883
CAS No.:945721-10-8
- 6-Aldehydo-7-methoxyiso-ophiopogonanone B
Catalog No.:BCC8345
CAS No.:123941-06-0
- (R)-(+)-m-Nitrobiphenyline oxalate
Catalog No.:BCC7525
CAS No.:945618-97-3
- Pexmetinib (ARRY-614)
Catalog No.:BCC6509
CAS No.:945614-12-0
- AMG-900
Catalog No.:BCC2175
CAS No.:945595-80-2
- Levcromakalim
Catalog No.:BCC7039
CAS No.:94535-50-9
- 9(11),12-Oleanadien-3-ol
Catalog No.:BCN4499
CAS No.:94530-87-7
- Senkyunolide G
Catalog No.:BCC9143
CAS No.:94530-85-5
- Senkyunolide E
Catalog No.:BCC9142
CAS No.:94530-83-3
- 20-Deoxocarnosol
Catalog No.:BCN3152
CAS No.:94529-97-2
- 3,4-Dihydro-6,7-(methylenedioxy)-2(1H)-quinolinone
Catalog No.:BCN1299
CAS No.:94527-34-1
- 4-Hydroxy-2-methoxyphenol 1-O-(6-O-syringoyl)glucoside
Catalog No.:BCN1300
CAS No.:945259-61-0
- AA 29504
Catalog No.:BCC7829
CAS No.:945828-50-2
- Parisyunnanoside B
Catalog No.:BCN2837
CAS No.:945865-37-2
- Senkyunolide H
Catalog No.:BCN6352
CAS No.:94596-27-7
- Senkyunolide I
Catalog No.:BCN6353
CAS No.:94596-28-8
- LX-1031
Catalog No.:BCC1712
CAS No.:945976-76-1
- RO5126766(CH5126766)
Catalog No.:BCC6374
CAS No.:946128-88-7
- Mulberrofuran K
Catalog No.:BCN7188
CAS No.:94617-36-4
- RN 1734
Catalog No.:BCC7770
CAS No.:946387-07-1
- LY2409881
Catalog No.:BCC5650
CAS No.:946518-60-1
- Hyperectine
Catalog No.:BCN3406
CAS No.:94656-46-9
- MNI 137
Catalog No.:BCC6156
CAS No.:946619-21-2
- Rhodiolgin; Gossypetin-7-O-α-rhamnopyranoside
Catalog No.:BCC8247
CAS No.:94696-39-6
Phase I evaluation of XL019, an oral, potent, and selective JAK2 inhibitor.[Pubmed:24374145]
Leuk Res. 2014 Mar;38(3):316-22.
This phase I study evaluated selective JAK2 inhibitor XL019 in 30 patients with myelofibrosis. The initial dose cohorts were 100, 200, and 300 mg orally on days 1-21 of a 28-day cycle. Central and/or peripheral neurotoxicity developed in all patients. Subsequently, patients were treated on lower doses; neurotoxicity was again observed, leading to study termination. Peripheral neuropathy resolved in 50%, and central neurotoxicity in all patients within months after therapy cessation. Myelosuppression was minimal. The terminal half-life of XL019 was approximately 21 h, with steady state reached by Day 8. International Working Group defined responses were seen in three (10%) patients.