MGCD-265Met/Flt/Flk/Ron/Tie-2 inhibitor CAS# 875337-44-3 |
- Tie2 kinase inhibitor
Catalog No.:BCC2561
CAS No.:948557-43-5
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 875337-44-3 | SDF | Download SDF |
PubChem ID | 24901704 | Appearance | Powder |
Formula | C26H20FN5O2S2 | M.Wt | 517.6 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : ≥ 100 mg/mL (193.20 mM) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | N-[[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-phenylacetamide | ||
SMILES | CN1C=C(N=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=CC=C5)F | ||
Standard InChIKey | UFICVEHDQUKCEA-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C26H20FN5O2S2/c1-32-14-20(29-15-32)23-13-19-25(36-23)22(9-10-28-19)34-21-8-7-17(12-18(21)27)30-26(35)31-24(33)11-16-5-3-2-4-6-16/h2-10,12-15H,11H2,1H3,(H2,30,31,33,35) | ||
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 | MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1, 2, 3 with IC50 values of 1 nM, 3 nM, 3 nM and 4 nM, respectively. | ||||||
Targets | c-Met | VEGFR1 | VEGFR2 | VEGFR3 | |||
IC50 | 1 nM | 3 nM | 3 nM | 4 nM |
MGCD-265 Dilution Calculator
MGCD-265 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.932 mL | 9.66 mL | 19.3199 mL | 38.6399 mL | 48.2998 mL |
5 mM | 0.3864 mL | 1.932 mL | 3.864 mL | 7.728 mL | 9.66 mL |
10 mM | 0.1932 mL | 0.966 mL | 1.932 mL | 3.864 mL | 4.83 mL |
50 mM | 0.0386 mL | 0.1932 mL | 0.3864 mL | 0.7728 mL | 0.966 mL |
100 mM | 0.0193 mL | 0.0966 mL | 0.1932 mL | 0.3864 mL | 0.483 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
MGCD-265 is a multi-target and ATP-competitive inhibitor of c-Met and VEGFR1, 2, 3 with IC50 values of 1 nM, 3 nM, 3 nM and 4 nM, respectively. [1]
In Non-small cell lung cancer xenograft models including one that harbored the TKI resistant EGFR mutation T790M, MGCD265 combined with either paclitaxel, docetaxel or erlotinib. Each combination elicited greater tumor response than agent alone, and displayed antiangiogenic properties with docetaxel [2].
MGCD265 has been studied in a variety of advanced solid tumors including NSCLC, as a monotherapy and in combination with either docetaxel or erlotinib. In a phase I study, MGCD265 was given orally from 24 mg/m2 daily to 235 mg/m2 twice daily uninterrupted to patients with advanced solid malignancy until disease progression [3]. In a phase I standard 3+3 dose escalation, MGCD265 (96 mg/m2 once daily up to 162 mg/m2 bid) was combined with erlotinib at 100 or 150 mg daily to determine safety, and 45 patients have been enrolled. In a separate phase I dose escalating trial, MGCD265 was combined with docetaxel (50 then 75 mg/m2 iv once every 3 weeks) in advanced solid tumors (n=34), including 9 NSCLC patients. The MTD of the microionized formulation of MGCD265 is 72 mg/m2 bid and docetaxel 75 mg/m2 every 3 weeks but has not been reached with the new formulation. [4][5]
References:
[1] Bonfils C. et al. AACR 2012 Annual Meeting, 2012. Abstract 1790.
[2]. Besterman JM, Fournel M, Dupont I, et al. Potent preclinical antitumor activity of MGCD265, an oral Met/VEGFR kinase inhibitor in phase II clinical development, in combination with taxanes or erlotinib. J Clin Oncol 2010;28:abstr e13595.
[3]. Kollmannsberger CK, Hurwitz H, Vlahovic G, et al. Phase I study of daily administration of MGCD265 to patients with advanced malignancies (Study 265-101). J Clin Oncol 2009;27:abstr e14525.
[4]. Kollmannsberger CK, Hurwitz H, Cleary JM, et al. MGCD265, a multitargeted oral tyrosine kinase receptor inhibitor of Met and VEGFR: Dose-escalation phase I study (abstr 3039). 2012 ASCO Annual Meeting Chicago, IL. J Clin Oncol 2012;30:abstr 3039.
[5]. Drouin MA, Kollmannsberger CK, Uronis HE, et al. Daily administration of MGCD265 to patients with solid tumors in a dose-escalation phase I study (study 265-101). J Clin Oncol 2010;28:abstr 3106.
- JNJ-26481585
Catalog No.:BCC2147
CAS No.:875320-29-9
- Dimethyl lithospermate B
Catalog No.:BCN2823
CAS No.:875313-64-7
- Lusianthridin
Catalog No.:BCN3689
CAS No.:87530-30-1
- YIL 781
Catalog No.:BCC7826
CAS No.:875258-85-8
- Tenacissoside X
Catalog No.:BCN8354
CAS No.:875057-87-7
- H-D-Phg-OH
Catalog No.:BCC3313
CAS No.:875-74-1
- Boc-D-Cys(Trt)-OH
Catalog No.:BCC3381
CAS No.:87494-13-1
- ZK 756326
Catalog No.:BCC7413
CAS No.:874911-96-3
- LY2183240
Catalog No.:BCC1718
CAS No.:874902-19-9
- L-741,742 hydrochloride
Catalog No.:BCC5696
CAS No.:874882-93-6
- Isamoltane hemifumarate
Catalog No.:BCC6879
CAS No.:874882-92-5
- Toceranib phosphate
Catalog No.:BCC2006
CAS No.:874819-74-6
- Anacetrapib (MK-0859)
Catalog No.:BCC2327
CAS No.:875446-37-0
- H-D-Tyr-OtBu
Catalog No.:BCC3136
CAS No.:87553-74-0
- ent-14,15-Dinor-13-oxolabda-8(17),11-dien-18-oic acid
Catalog No.:BCN1319
CAS No.:875585-30-1
- Randaiol
Catalog No.:BCN4002
CAS No.:87562-14-9
- Kelampayoside A
Catalog No.:BCN4422
CAS No.:87562-76-3
- PPY A
Catalog No.:BCC3895
CAS No.:875634-01-8
- cis-3,4-Dihydroxy-beta-ionone
Catalog No.:BCN6694
CAS No.:875666-39-0
- LXR-623
Catalog No.:BCC4273
CAS No.:875787-07-8
- (+)-Lyoniresinol 9'-O-glucoside
Catalog No.:BCN4832
CAS No.:87585-32-8
- Smyrindioloside
Catalog No.:BCN4423
CAS No.:87592-77-6
- Ptaquiloside
Catalog No.:BCN8159
CAS No.:87625-62-5
- Montixanthone
Catalog No.:BCN8069
CAS No.:876305-36-1