Glesatinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Glesatinib (MGCD-265) 是一种酪氨酸激酶抑制剂，可有效、选择性地抑制 Met 和 Axl 激酶。

Glesatinib (MGCD-265) is a tyrosine kinase inhibitor that potently and selectively inhibits Met and Axl kinase.Lung Cancer Phase 2 Clinical.

Glesatinib (MGCD265; 0.01-5 μM; for 72 hours) results in a dose-dependent inhibition of cancer cell growth and shows the low IC50 value of 0.08 μM on NSCLC H1299 cells. Glesatinib (0.01, 0.1, 0.5, 1 μM) significantly increases by several-fold the percentage of apoptotic cells in NSCLC H1299 cells. Glesatinib has the cytotoxicity to P-gp overexpressing cancer cells KB-C2, SW620/Ad300, HEK293/ABCB1, and their parent cells KB-3-1, SW620, HEK293 cells with the IC50s fell between 5 and 10 μM. Glesatinib (1, 3 μM; 120 mins) increases the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp. Glesatinib (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner. Cell Proliferation Assay Cell Line:NSCLC H1299 cells Concentration:0.01, 0.1, 1, 2, 5 μM Incubation Time:For 72 hoursResult:Resulted in a dose-dependent inhibition of cancer cell growth and showed the lowest IC50 value of 0.08 μM.

Glesatinib (MGCD265; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size. Animal Model:4?6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts Dosage:15 mg/kg Administration:Orally; daily; 40 weeks Result:Caused a significant decrease in tumor size.

MGCD-265 | MGCD265 | MGCD 265

Angiogenesis

c-Met/HGFR

c-Met/HGFR

Cancer

Lung Cancer

936694-12-1

619.71

C31H27F2N5O3S2

>98% (HPLC)

——

O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=NC=C(CNCCOC)C=C4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=C(F)C=C5

N-((3-fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)carbamothioyl)-2-(4-fluorophenyl)acetamide

(-20℃)

With Ice Pack

≥ 2 years