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MGCD-265 is an inhibitor of c-Met and VEGFR2 (IC50s = 0.029 and 0.01 µM, respectively). It is selective for c-Met and VEGFR2 over Chk1, EGFR, GSK3beta, IGF-1R, IKKbeta, JAK2, and JNK1 at 0.1 µM but also inhibits VEGFR1, VEGFR3, Ron, Tie2, FLT3, c-Kit, Abl, and TrkA with percent inhibition values ranging from 80 to 100% at 0.1 µM. MGCD-265 also binds to Smoothened (Smo) in HEK293T cell membranes expressing the human receptor (Ki = 0.0417 µM for the wild-type receptor) and inhibits Gli1-mediated transcription in a reporter assay in gefitinib-resistant HCC827 non-small cell lung cancer (NSCLC) cells. It inhibits migration of A549 NSCLC cells induced by hepatocyte growth factor (HGF) and VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs, IC50s = 2 and 0.025 µM, respectively). MGCD-265 (20 mg/kg) reduces tumor growth in several mouse xenograft models, including prostate, colorectal, and gastric cancer models.Formal Name: N-[[[3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-benzeneacetamide. CAS Number: 875337-44-3. Molecular Formula: C26H20FN5O2S2. Formula Weight: 517.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml. lambdamax: 258, 311 nm. 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. InChi Code: 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). InChi Key: UFICVEHDQUKCEA-UHFFFAOYSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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