Glesatinib (hydrochloride)
Glesatinib (hydrochloride) Basic information
- Product Name:
- Glesatinib (hydrochloride)
- Synonyms:
-
- Glesatinib (hydrochloride)
- Glesatinib HCl
- MGCD-265 HYDROCHLORIDE
- CS-2642
- Glesatinib (hydrochloride)(MGCD265 hydrochloride)
- CAS:
- 1123838-51-6
- MF:
- C31H28ClF2N5O3S2
- MW:
- 656.16
- Mol File:
- 1123838-51-6.mol
Glesatinib (hydrochloride) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 28 mg/mL (42.67 mM)
- form
- Solid
- color
- Off-white to pink
Glesatinib (hydrochloride) Usage And Synthesis
Description
Glesatinib HCl is a novel potent MET/SMO dual inhibitor.
Uses
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)[1][2].
in vivo
Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size[1].
| Animal Model: | 4?6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts[1] |
| Dosage: | 15 mg/kg |
| Administration: | Orally; daily; 40 weeks |
| Result: | Caused a significant decrease in tumor size. |
References
[1] Morgillo F, et al. Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. J Med Chem. 2017 Sep 14;60(17):7447-7458. DOI:10.1021/acs.jmedchem.7b00794
[2] Cui Q, et al. Glesatinib, a c-MET/SMO Dual Inhibitor, Antagonizes P-glycoprotein Mediated MultidrugResistance in Cancer Cells. Front Oncol. 2019 Apr 25;9:313. DOI:10.3389/fonc.2019.00313
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