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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

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About This Item

Empirical Formula (Hill Notation):
C20H25F3N8O4
CAS Number:
2067281-51-8
Molecular Weight:
498.46
UNSPSC Code:
12352107
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

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

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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