[CAS NO. 1116743-46-4] SAR125844

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PRODUCTS SPECIFICATIONS [1116743-46-4]

Catalog

HY-16446

Brand

MCE

CAS

1116743-46-4

DESCRIPTION [1116743-46-4]

Overview

MDL	MFCD25976852
Molecular Weight	550.63
Molecular Formula	C25H23FN8O2S2
SMILES	O=C(NCCN1CCOCC1)NC2=NC3=CC=C(SC4=NN=C5C=CC(C6=CC=C(F)C=C6)=NN54)C=C3S2

For research use only. We do not sell to patients.

Summary

SAR125844 is a potent, highly selective, reversible and ATP-competitive MET receptor tyrosine kinase (RTK) inhibitor, with an IC ₅₀ of 4.2 nM. Shows inhibition of MET autophosphorylation in cell-based assays ^[1] .

IC50 & Target

IC50: 4.2 nM (MET RTK) ^[1] .

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01657214	Sanofi	Neoplasm Malignant	September 2012	Phase 1
NCT02435121	Sanofi	Neoplasm Malignant	November 2015	Phase 2
NCT01391533	Sanofi	Malignant Solid Tumors	July 2011	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 45 mg/mL ( 81.72 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8161 mL	9.0805 mL	18.1610 mL
5 mM	0.3632 mL	1.8161 mL	3.6322 mL
10 mM	0.1816 mL	0.9081 mL	1.8161 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.25 mg/mL (4.09 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Egile C, et al. The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer. Mol Cancer Ther. 2015 Feb;14(2):384-94.