Glesatinib HCl

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 464760

CAS#: 1123838-51-6 (HCl)

Description: Glesatinib HCl is a novel potent MET/SMO dual inhibitor.

Chemical Structure

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Glesatinib HCl
CAS# 1123838-51-6 (HCl)
Instruction

Theoretical Analysis

MedKoo Cat#: 464760
Name: Glesatinib HCl
CAS#: 1123838-51-6 (HCl)
Chemical Formula: C31H28ClF2N5O3S2
Exact Mass: 0.00
Molecular Weight: 656.164
Elemental Analysis: C, 56.75; H, 4.30; Cl, 5.40; F, 5.79; N, 10.67; O, 7.31; S, 9.77

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Related CAS #: 1123838-51-6 (HCl)   936694-12-1 (free base)   Glesatinib Glycolate  

Synonym: Glesatinib HCl; Glesatinib hydrochloride; MGCD265 hydrochloride; MGCD265 hydrochloride; MGCD265 hydrochloride; MGCD265 HCl; MGCD 265 HCl; MGCD-265 HCl;

IUPAC/Chemical Name: 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 hydrochloride

InChi Key: TUVXGVPWXBWWEP-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: 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.[H]Cl

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 656.16 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Huang C, Zou Q, Liu H, Qiu B, Li Q, Lin Y, Liang Y. Management of Non-small Cell Lung Cancer Patients with MET Exon 14 Skipping Mutations. Curr Treat Options Oncol. 2020 Apr 18;21(4):33. doi: 10.1007/s11864-020-0723-5. PMID: 32306194.

2: Cui Q, Cai CY, Gao HL, Ren L, Ji N, Gupta P, Yang Y, Shukla S, Ambudkar SV, Yang DH, Chen ZS. Glesatinib, a c-MET/SMO Dual Inhibitor, Antagonizes P-glycoprotein Mediated Multidrug Resistance in Cancer Cells. Front Oncol. 2019 Apr 25;9:313. doi: 10.3389/fonc.2019.00313. PMID: 31106148; PMCID: PMC6494935.

3: Morgillo F, Amendola G, Della Corte CM, Giacomelli C, Botta L, Di Maro S, Messere A, Ciaramella V, Taliani S, Marinelli L, Trincavelli ML, Martini C, Novellino E, Ciardiello F, Cosconati S. 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. Epub 2017 Aug 22. PMID: 28787156.

4: Engstrom LD, Aranda R, Lee M, Tovar EA, Essenburg CJ, Madaj Z, Chiang H, Briere D, Hallin J, Lopez-Casas PP, Baños N, Menendez C, Hidalgo M, Tassell V, Chao R, Chudova DI, Lanman RB, Olson P, Bazhenova L, Patel SP, Graveel C, Nishino M, Shapiro GI, Peled N, Awad MM, Jänne PA, Christensen JG. Glesatinib Exhibits Antitumor Activity in Lung Cancer Models and Patients Harboring MET Exon 14 Mutations and Overcomes Mutation-mediated Resistance to Type I MET Inhibitors in Nonclinical Models. Clin Cancer Res. 2017 Nov 1;23(21):6661-6672. doi: 10.1158/1078-0432.CCR-17-1192. Epub 2017 Aug 1. PMID: 28765324.

5: Reungwetwattana T, Liang Y, Zhu V, Ou SI. The race to target MET exon 14 skipping alterations in non-small cell lung cancer: The Why, the How, the Who, the Unknown, and the Inevitable. Lung Cancer. 2017 Jan;103:27-37. doi: 10.1016/j.lungcan.2016.11.011. Epub 2016 Nov 15. PMID: 28024693.