A multi-kinase inhibitor; inhibits Axl and c-MET (IC50s = 7 and 12 nM

CEP-40783 – 5 mg

Brand:
Cayman
CAS:
1437321-24-8
Storage:
-20
UN-No:
Non-Hazardous - /

CEP-40783 is an inhibitor of the receptor tyrosine kinases Axl and c-MET (IC50s = 7 and 12 nM, respectively).{43937} It inhibits Axl in 293GT cells expressing Axl and c-MET in NCI H1299 non-small cell lung cancer (NSCLC) cells with IC50 values of 0.26 and 6 nM, respectively. It also inhibits the receptor tyrosine kinases TYRO3 and MER (IC50s = 3.5 and 1.89 nM, respectively).{43938} CEP-40783 (0.3 mg/kg) induces complete regression of tumors in an Axl/NIH3T3 mouse xenograft model and reduces the metastatic tumor burden in mouse orthotopic breast cancer models. It also induces tumor stasis and regression in an EBC-1 NSCLC mouse xenograft model when administered at doses of 3 and 10 mg/kg, respectively. CEP-40783 reduces tumor growth in an MC38 mouse syngeneic model concomitantly with an increase in leukocyte infiltration into tumors, the production of IFN-γ in natural killer cells, and the percentage of CD8+ T cells in tumor tissue.{43938}  

 

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SKU: 25749 - 5 mg Category:

Description

A multi-kinase inhibitor; inhibits Axl and c-MET (IC50s = 7 and 12 nM, respectively); inhibits Axl in 293GT cells expressing Axl and c-MET in NCI H1299 NSCLC cells (IC50s = 0.26 and 6 nM, respectively); inhibits TYRO3 and MER (IC50s = 3.5 and 1.89 nM, respectively); induces complete regression of tumors in an Axl/NIH3T3 mouse xenograft model at 0.3 mg/kg; induces tumor stasis and regression in an EBC-1 NSCLC mouse xenograft model at 3 and 10 mg/kg, respectively; reduces tumor growth in an MC38 mouse syngeneic model concomitantly with innate and adaptive immune cell activation

Formal name: N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-3-fluorophenyl]-3-(4-fluorophenyl)-1,2,3,4-tetrahydro-1-(1-methylethyl)-2,4-dioxo-5-pyrimidinecarboxamide

Synonyms:  RXDX-106

Molecular weight: 588.6

CAS: 1437321-24-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling

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