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MGCD-265
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MGCD-265图片
CAS NO:875337-44-3
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍
MGCD-265 是一种有效的口服活性 c-Met 和 VEGFR2 酪氨酸激酶抑制剂，IC50 分别为 29 nM 和 10 nM。 MGCD-265 具有显着的抗肿瘤活性。
Cas No.875337-44-3
别名N-(3-氟-4-(2-(1-甲基-1H-咪唑-4-基)噻吩并[3,2-B]吡啶-7-氧基)苯基氨基硫代甲酰基)-2-苯乙酰胺
化学名N-[[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-phenylacetamide
Canonical SMILESCN1C=C(N=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=CC=C5)F
分子式C26H20FN5O2S2
分子量517.6
溶解度≥ 25.9mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.