S-49076 | CAS#1265965-22-7 | MET, AXL/MER | FGFR1/2/3

MedKoo Cat#: 206484 | Name: S-49076

Description:

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

S-49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3. A phase I study with S-49076 is currently underway in patients with advanced solid tumors.

Chemical Structure

S-49076

CAS# 1265965-22-7 (free base)

Theoretical Analysis

MedKoo Cat#: 206484

Name: S-49076

CAS#: 1265965-22-7 (free base)

Chemical Formula: C22H22N4O4S

Exact Mass: 438.1362

Molecular Weight: 438.50

Elemental Analysis: C, 60.26; H, 5.06; N, 12.78; O, 14.59; S, 7.31

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 500.00	2 Weeks
50mg	USD 950.00	2 Weeks

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Related CAS #

1265965-19-2 (HCl) 1265965-22-7 (free base)

Synonym

S-49076; S49076; S 49076.

IUPAC/Chemical Name

(Z)-3-((3-((4-(morpholinomethyl)-1H-pyrrol-2-yl)methylene)-2-oxoindolin-5-yl)methyl)thiazolidine-2,4-dione

InChi Key

AREYWCZYVPSHGS-NVMNQCDNSA-N

InChi Code

InChI=1S/C22H22N4O4S/c27-20-13-31-22(29)26(20)12-14-1-2-19-17(8-14)18(21(28)24-19)9-16-7-15(10-23-16)11-25-3-5-30-6-4-25/h1-2,7-10,23H,3-6,11-13H2,(H,24,28)/b18-9-

SMILES Code

O=C(N1CC2=CC3=C(NC(/C3=C\C4=CC(CN5CCOCC5)=CN4)=O)C=C2)SCC1=O

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

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

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

Related CAS# 1265965-22-7(S-49076 Free Base) 1265966-31-1(722572

Product Data

Product Data

Instruction

View handling instruction

	Solvent	mg/mL	mM
Solubility
	DMSO	87.0	198.40

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 438.50 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.

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:

1. Clémenson C, Chargari C, Liu W, Mondini M, Ferté C, Burbridge MF, Cattan V, Jacquet-Bescond A, Deutsch E. The MET/AXL/FGFR Inhibitor S49076 Impairs Aurora B Activity and Improves the Antitumor Efficacy of Radiotherapy. Mol Cancer Ther. 2017 Oct;16(10):2107-2119. doi: 10.1158/1535-7163.MCT-17-0112. Epub 2017 Jun 15. PMID: 28619752. 2. Burbridge MF, Bossard CJ, Saunier C, Fejes I, Bruno A, Léonce S, Ferry G, Da Violante G, Bouzom F, Cattan V, Jacquet-Bescond A, Comoglio PM, Lockhart BP, Boutin JA, Cordi A, Ortuno JC, Pierré A, Hickman JA, Cruzalegui FH, Depil S. S49076 is a novel kinase inhibitor of MET, AXL, and FGFR with strong preclinical activity alone and in association with bevacizumab. Mol Cancer Ther. 2013 Sep;12(9):1749-62. doi: 10.1158/1535-7163.MCT-13-0075. Epub 2013 Jun 26. PMID: 23804704. 3. Tosca EM, Gauderat G, Fouliard S, Burbridge M, Chenel M, Magni P. Modeling restoration of gefitinib efficacy by co-administration of MET inhibitors in an EGFR inhibitor-resistant NSCLC xenograft model: A tumor-in-host DEB-based approach. CPT Pharmacometrics Syst Pharmacol. 2021 Nov;10(11):1396-1411. doi: 10.1002/psp4.12710. Epub 2021 Oct 28. PMID: 34708556; PMCID: PMC8592518. 4. Rodon J, Postel-Vinay S, Hollebecque A, Nuciforo P, Azaro A, Cattan V, Marfai L, Sudey I, Brendel K, Delmas A, Malasse S, Soria JC. First-in-human phase I study of oral S49076, a unique MET/AXL/FGFR inhibitor, in advanced solid tumours. Eur J Cancer. 2017 Aug;81:142-150. doi: 10.1016/j.ejca.2017.05.007. PMID: 28624695.

In vitro protocol:

In vivo protocol:

1. Tosca EM, Gauderat G, Fouliard S, Burbridge M, Chenel M, Magni P. Modeling restoration of gefitinib efficacy by co-administration of MET inhibitors in an EGFR inhibitor-resistant NSCLC xenograft model: A tumor-in-host DEB-based approach. CPT Pharmacometrics Syst Pharmacol. 2021 Nov;10(11):1396-1411. doi: 10.1002/psp4.12710. Epub 2021 Oct 28. PMID: 34708556; PMCID: PMC8592518. 2. Rodon J, Postel-Vinay S, Hollebecque A, Nuciforo P, Azaro A, Cattan V, Marfai L, Sudey I, Brendel K, Delmas A, Malasse S, Soria JC. First-in-human phase I study of oral S49076, a unique MET/AXL/FGFR inhibitor, in advanced solid tumours. Eur J Cancer. 2017 Aug;81:142-150. doi: 10.1016/j.ejca.2017.05.007. PMID: 28624695.

1: Burbridge MF, Bossard CJ, Saunier C, Fejes I, Bruno A, Léonce S, Ferry G, Da Violante G, Bouzom F, Cattan V, Jacquet-Bescond A, Comoglio PM, Lockhart BP, Boutin JA, Cordi A, Ortuno JC, Pierré A, Hickman JA, Cruzalegui FH, Depil S. S49076 is a novel kinase inhibitor of MET, AXL, and FGFR with strong preclinical activity alone and in association with bevacizumab. Mol Cancer Ther. 2013 Sep;12(9):1749-62. doi: 10.1158/1535-7163.MCT-13-0075. Epub 2013 Jun 26. PubMed PMID: 23804704. 2: Postel-Vinay, S., Hollebecque, A., Soria, J. C., Balandraud, S., Brendel, K., Cattan, V., ... & Rodon, J. (2015). 125O First-in-human study of oral S 49076, a MET/AXL/FGFR inhibitor, in advanced solid tumors. Annals of Oncology, 26, ix37. 3: Park, K., Ciardiello, F., Hida, T., Lim, W., Lin, C. C., Murakami, H., ... & Paz-Ares, L. (2017). Phase I/II study of S 49076, a MET/AXL/FGFR inhibitor, in combination with gefitinib in EGFR-mutated NSCLC patients who progress on EGFR tyrosine kinase inhibitor. Annals of Oncology, 28, v493.