SML3217

PF-06843195

≥98% (HPLC), storage temp.:2-8°C

• Synonym(s): 2,2-Difluoroethyl (3S)-3-[[2′-amino-5-fluoro-2-(4-morpholinyl)[4,5′-bipyrimidin]-6-yl]amino]-3-(hydroxymethyl)-1-pyrrolidinecarboxylate, PF 06843195, PF 06862309 active drug, PF-06862309 active drug, PF06843195
• Empirical Formula (Hill Notation): C₂₀H₂₅F₃N₈O₄
• CAS Number: 2067281-51-8
• Molecular Weight: 498.46
• UNSPSC Code: 12352107
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: OC[C@]1(CN(CC1)C(OCC(F)F)=O)NC2=NC(N3CCOCC3)=NC(C4=CN=C(N)N=C4)=C2F
• InChI key: RTOREZYNLPQUKM-FQEVSTJZSA-N

Description

Biochem/physiol Actions

PF-06843195 is a potent and PI3K-alpha subtype-selective phosphoinositide 3-kinase (PI3K) inhibitor (rat PI3K Ki = 2 nM/β, <18 nM/α, <280 nM/δ) that inhibits cellular PI3Kα activity at a higher potency over that of PI3Kδ/β and mTOR (AKT pT308 IC50 = 18/160/360 nM in rat PI3Kα/δ/β Rat1 lines; p70S6K pT389 IC50 = 1.5 μM in Rat1 myristoylated PI3K line). PF-06843195 is more potent against cellular AKT pT308 (MCF7/T47D IC50 = 7.8/8.7 nM) and proliferation (MCF7/T47D = 62/32 nM) than alpelisib (BYL719) in cultures.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable