Glesatinib hydrochloride

Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).

Product information

CAS Number: 1123838-51-6

Molecular Weight: 656.17

Formula: C31H28ClF2N5O3S2

Chemical Name: 3-(3-fluoro-4-{[2-(5-{[(2-methoxyethyl)amino]methyl}pyridin-2-yl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)-1-[2-(4-fluorophenyl)acetyl]thiourea hydrochloride

Smiles: Cl.COCCNCC1C=CC(=NC=1)C1=CC2N=CC=C(OC3=CC=C(C=C3F)NC(=S)NC(=O)CC3C=CC(F)=CC=3)C=2S1

InChiKey: TUVXGVPWXBWWEP-UHFFFAOYSA-N

InChi: InChI=1S/C31H27F2N5O3S2.ClH/c1-40-13-12-34-17-20-4-8-24(36-18-20)28-16-25-30(43-28)27(10-11-35-25)41-26-9-7-22(15-23(26)33)37-31(42)38-29(39)14-19-2-5-21(32)6-3-19;/h2-11,15-16,18,34H,12-14,17H2,1H3,(H2,37,38,39,42);1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (76.20 mM; Need ultrasonic). H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

Products are for research use only. Not for human use.