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Glesatinib hydrochloride

CAS No. : 1123838-51-6

MCE 国际站：Glesatinib hydrochloride

产品活性：Glesatinib hydrochloride (MGCD265 hydrochloride) 是一种具有口服活性的，有效的 MET/SMO 双抑制剂。 Glesatinib hydrochloride 是一种酪氨酸激酶抑制剂，可拮抗非小细胞肺癌 (NSCLC) 中 P 糖蛋白介导的多药耐药性 (MDR)。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：TAM Receptor | c-Met/HGFR

In Vitro: 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.

In Vivo: Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size.

相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Anti-Lung Cancer Compound Library | 2-D08 | PHA-665752 | 2-Phospho-L-ascorbic acid trisodium | SGI⁻⁷079 | SU11274 | SRI 31215 TFA | c-Met inhibitor 1 | X-376 | TAM-IN-2 | Tyrosine kinase inhibitor | c-met-IN-1 | Meleagrin | Norleual | RU-302 | Ensartinib

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