MGCD-265

Met/Flt/Flk/Ron/Tie-2 inhibitor CAS# 875337-44-3

MGCD-265

Catalog No. BCC2479----Order now to get a substantial discount!

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MGCD-265: 5mg $138 In Stock
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Chemical structure

MGCD-265

3D structure

Chemical Properties of MGCD-265

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.

Biological Activity of MGCD-265

DescriptionMGCD-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.
Targetsc-MetVEGFR1VEGFR2VEGFR3    
IC501 nM3 nM3 nM4 nM    

MGCD-265 Dilution Calculator

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MGCD-265 Molarity Calculator

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Preparing Stock Solutions of MGCD-265

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.

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Calcutta University

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The University of Tokyo
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Korea University
Korea University

Background on MGCD-265

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.

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Description

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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