An inhibitor of Axl (IC50 = 27 nM ); exhibits greater than 50% inhibition of 11 kinases

TP-0903 – 5 mg

Brand:
Cayman
CAS:
1341200-45-0
Storage:
-20
UN-No:
Non-Hazardous - /

TP-0903 is an inhibitor of the receptor tyrosine kinase Axl (IC50 = 27 nM ).{53037} It exhibits greater than 50% inhibition of 11 kinases, including MER, TYRO3, JAK2, ALK, and Abl1, in a panel of 75 kinases at 200 nM, with IC50 values of 3 and 12.4 nM for Aurora A and B, respectively. TP-0903 decreases the phosphorylation of Akt and Axl in GAS6-stimulated, serum-starved PSN-1 pancreatic cancer cells (EC50s = 305 and 222 nM, respectively). It decreases cell viability (IC50 = 6 nM) and induces cell cycle arrest at the G2/M phase in PSN-1 cells when used at a concentration of 30 nM. TP-0903 also reduces the viability of colorectal cancer (CRC) cell lines with IC50 values ranging from 4.5 to 123 nM.{53038} It exhibits 69 and 44% tumor growth inhibition in an HCT116 mouse xenograft model and a K-Ras-mutant CRC patient-derived xenograft (PDX) mouse model, respectively, when administered at a dose of 40 mg/kg.  

 

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SKU: 28757 - 5 mg Category:

Description

An inhibitor of Axl (IC50 = 27 nM ); exhibits greater than 50% inhibition of 11 kinases, including MER, TYRO3, JAK2, ALK, and Abl1, in a panel of 75 kinases at 200 nM, with IC50 values of 3 and 12.4 nM for Aurora A and B, respectively; decreases the phosphorylation of Akt and Axl in GAS6-stimulated, serum-starved PSN-1 pancreatic cancer cells (EC50s = 305 and 222 nM, respectively); decreases cell viability (IC50 = 6 nM) and induces cell cycle arrest at the G2/M phase in PSN-1 cells at 30 nM; reduces the viability of CRC cell lines (IC50s = 4.5-123 nM); exhibits 69 and 44% tumor growth inhibition in an HCT116 mouse xenograft model and a K-Ras-mutant CRC PDX mouse model, respectively, at 40 mg/kg

Formal name: 2-[[5-chloro-2-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-4-pyrimidinyl]amino]-N,N-dimethyl-benzenesulfonamide

Synonyms: 

Molecular weight: 516.1

CAS: 1341200-45-0

Purity: ≥98%

Formulation: A crystalline solid

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