Glesatinib hydrochloride

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 hydrochloride (MGCD265 hydrochloride; 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 hydrochloride (0.01, 0.1, 0.5, 1 μM) significantly increases by several-fold the percentage of apoptotic cells in NSCLC H1299 cells. Glesatinib hydrochloride 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 hydrochloride (1, 3 μM; 120 mins) increases the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp. Glesatinib hydrochloride (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner.

Glesatinib hydrochloride (MGCD265 hydrochloride; 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 hydrochloride

Tyrosine Kinase

TAM Receptor

TAM Receptor

Cancer

Lung Cancer

1123838-51-6

655.1576

C31H27ClF2N5O3S2X

>98% (HPLC)

DMSO: ≥ 28 mg/mL

COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=C(C=C5)F)F.Cl

Benzeneacetamide, 4-fluoro-N-[[[3-fluoro-4-[[2-[5-[[(2-methoxyethyl)amino]methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-, hydrochloride (1:x)

(-20℃)

With Ice Pack

≥ 2 years