839707-37-8

Basic information

• Product Name: N-(3-(7-(1,3-dimethyl-1H-pyrazol-5-ylamino)-1-methyl-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)-4-methylphenyl)-3-(trifluoromethyl)benzamide
• Synonyms: SC1 (Pluripotin);N-(3-(7-((1,3-Dimethyl-1H-pyrazol-5-yl)amino)-1-methyl-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimid;N-(3-(7-(1,3-dimethyl-1H-pyrazol-5-ylamino)-1-methyl-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)-4-methylphenyl)-3-(trifluoromethyl)benzamide;Pluripotin;Pluripotin (SC-1);N-[3-[7-[(1,3-Dimethyl-1H-pyrazol-5-yl)amino]-1,4-dihydro-1-methyl-2-oxopyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide;N-[3-[7-(2,5-Dimethyl-2H-pyrazol-3-ylamino)-1-methyl-2-oxo-1,4-dihydro-2H-pyrimido[4,5-d]pyrimidin-3-yl]-4-methylphenyl]-3-trifluoromethyl-benzamide
• CAS NO: 839707-37-8
• Molecular Formula: C27H25F3N8O2
• Molecular Weight: 551
• EINECS: -0
• Product Categories: Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals
• Mol File: 839707-37-8.mol
• Article Data: 1

Chemical Properties

• Appearance: white to beige/
• Density: 1.43
• Storage Temp.: ?20°C
• Solubility: DMSO: soluble10mg/mL (clear solution)
• CAS DataBase Reference: N-(3-(7-(1,3-dimethyl-1H-pyrazol-5-ylamino)-1-methyl-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)-4-methylphenyl)-3-(trifluoromethyl)benzamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(3-(7-(1,3-dimethyl-1H-pyrazol-5-ylamino)-1-methyl-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)-4-methylphenyl)-3-(trifluoromethyl)benzamide(839707-37-8)
• EPA Substance Registry System: N-(3-(7-(1,3-dimethyl-1H-pyrazol-5-ylamino)-1-methyl-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)-4-methylphenyl)-3-(trifluoromethyl)benzamide(839707-37-8)

Safety Data

• Hazard Codes: T
• Statements: 25
• Safety Statements: 45
• WGK Germany: 3
• Hazardous Substances Data: 839707-37-8(Hazardous Substances Data)

Usage

Uses

Pluripotin is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. Pluripotin has been shown to maintain embryonic stem cell (ESC) self-renewal. When combined with leukemia inhibitory factor, Pluripotin greatly promotes derivation of embryonic stem cell lines from refractory strains.

Upstream product

• 7627-38-5 2,4-dichloro-5-(chloromethyl)pyrimidine 
• 4433-40-3 5-(hydroxymethyl)pyrimidine-2,4-diol 

Relevant articles and documents

First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia

GNF-7, a multitargeted kinase inhibitor, served as a dual kinase inhibitor of ACK1 and GCK, which provided a novel therapeutic strategy for overriding AML expressing NRAS mutation. This SAR study with GNF-7 derivatives, designed to target NRAS mutant-driven AML, led to identification of the extremely potent inhibitors, 10d, 10g, and 11i, which possess single-digit nanomolar inhibitory activity against both ACK1 and GCK. These substances strongly suppress proliferation of mutant NRAS expressing AML cells via apoptosis and AKT/mTOR signaling blockade. Compound 11i is superior to GNF-7 in terms of kinase inhibitory activity, cellular activity, and differential cytotoxicity. Moreover, 10k possessing a favorable mouse pharmacokinetic profile prolonged life-span of Ba/F3-NRAS-G12D injected mice and significantly delayed tumor growth of OCI-AML3 xenograft model without causing the prominent level of toxicity found with GNF-7. Taken together, this study provides insight into the design of novel ACK1 and GCK dual inhibitors for overriding NRAS mutant-driven AML.