A c-Met inhibitor
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SAR125844

Item No. 37542

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[6-[[6-(4-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-2-benzothiazolyl]-N′-[2-(4-morpholinyl)ethyl]-urea
CAS Number
1116743-46-4
Molecular Formula
C25H23FN8O2S2
Formula Weight
550.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: Slightly SolubleDMSO: Slightly Soluble
λmax
228, 282 nm
SMILES
O=C(NCCN1CCOCC1)NC2=NC3=CC=C(C=C3S2)SC4=NN=C5C=CC(C6=CC=C(F)C=C6)=NN45
InChi Code
InChI=1S/C25H23FN8O2S2/c26-17-3-1-16(2-4-17)19-7-8-22-30-31-25(34(22)32-19)37-18-5-6-20-21(15-18)38-24(28-20)29-23(35)27-9-10-33-11-13-36-14-12-33/h1-8,15H,9-14H2,(H2,27,28,29,35)
InChi Key
ODIUNTQOXRXOIV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    SAR125844 is an inhibitor of the receptor tyrosine kinase c-Met (IC50 = 4 nM).1 It is selective for c-Met over tropomyosin-related kinase A (TrkA), TrkB, PDGFRα, Axl, and Mer (IC50s = 39, 280, 55, 87, and 105 nM, respectively).2 SAR125844 inhibits the proliferation of MKN45 gastric cancer cells (IC50 = 7 nM).1 In vivo, SAR125844 (20 mg/kg) inhibits intratumoral c-Met phosphorylation in a MET-amplified Hs 746T gastric cancer mouse xenograft model. SAR125844 (10-45 mg/kg) also reduces tumor volume in Hs 746T and SNU-5 gastric cancer mouse xenograft models.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ugolini, A., Kenigsberg, M., Rak, A., et al. Discovery and pharmacokinetic and pharmacological properties of the potent and selective MET kinase inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844). J. Med. Chem. 59(15), 7066-7074 (2016).

    2. Egile, C., Kenigsberg, M., Delaisi, C., et al. The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer. Mol. Cancer Ther. 14(2), 384-394 (2015).