A multi-kinase inhibitor; inhibits a variety of kinases

RGB-286638 – 500 mg

Brand:
Cayman
CAS:
784210-88-4
Storage:
-20
UN-No:
Non-Hazardous - /

RGB-286638 is a multi-kinase inhibitor.{47793} It inhibits a variety of kinases, including cyclin-dependent kinase 1 (CDK1), CDK2-7 and CDK9, as well as the tyrosine kinases FMS, JAK2, and c-Src and the serine/threonine kinases GSK3β, TAK1, JNK1A1, JNK1A2, AMPK, and MEK1 (IC50s = 1-55 nM). RGB-286638 inhibits proliferation of multiple myeloma cancer cell lines endogenously expressing mutant and wild-type p53 (EC50s = 20-70 nM), as well as patient-derived multiple myeloma cells when used at concentrations of 50 and 100 nM. It induces G1/S and G2/M cell cycle arrest and apoptosis of MM.1S human multiple myeloma cells when used at a concentration of 50 nM. RGB-286638 decreases tumor growth in an MM.1S mouse xenograft model when administered at doses of 30 and 40 mg/kg per day for 14 days.  

 

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SKU: 29499 - 500 mg Category:

Description

A multi-kinase inhibitor; inhibits a variety of kinases, including CDK2-7 and CDK9, FMS, JAK2, c-Src, GSK3β, TAK1, JNK1A1, JNK1A2, AMPK, and MEK1 (IC50s = 1-55 nM); inhibits proliferation of multiple myeloma cancer cell lines endogenously expressing mutant and wild-type p53 (EC50s = 20-70 nM), as well as patient-derived multiple myeloma cells at 50 and 100 nM; induces G1/S and G2/M cell cycle arrest and apoptosis of MM.1S human multiple myeloma cells at 50 nM; decreases tumor growth in an MM.1S mouse xenograft model at 30 and 40 mg/kg per day for 14 days

Formal name: N-[1,4-dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N′-4-morpholinyl-urea

Synonyms: 

Molecular weight: 545.6

CAS: 784210-88-4

Purity: ≥98%

Formulation: A crystalline solid

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