SML3217
PF-06843195
≥98% (HPLC), storage temp.:2-8°C
别名:
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
InChI key
RTOREZYNLPQUKM-FQEVSTJZSA-N
SMILES string
OC[C@]1(CN(CC1)C(OCC(F)F)=O)NC2=NC(N3CCOCC3)=NC(C4=CN=C(N)N=C4)=C2F
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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