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Merck
CN

PZ0281

PF-05212384

≥98% (HPLC)

Synonym(s):

1-(4-((4-(Dimethylamino)piperidin-1-yl)carbonyl)phenyl)-3-(4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl)urea, Gedatolisib, PKI-587

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About This Item

Empirical Formula (Hill Notation):
C32H41N9O4
CAS Number:
1197160-78-3
Molecular Weight:
615.73
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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SMILES string

N6(CCOCC6)c1nc(nc(n1)c3ccc(cc3)NC(=O)Nc4ccc(cc4)C(=O)N5CCC(CC5)N(C)C)N2CCOCC2

InChI

1S/C32H41N9O4/c1-38(2)27-11-13-39(14-12-27)29(42)24-5-9-26(10-6-24)34-32(43)33-25-7-3-23(4-8-25)28-35-30(40-15-19-44-20-16-40)37-31(36-28)41-17-21-45-22-18-41/h3-10,27H,11-22H2,1-2H3,(H2,33,34,43)

InChI key

DWZAEMINVBZMHQ-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 0.5 mg/mL, clear (warmed)

storage temp.

room temp

Quality Level

100

Biochem/physiol Actions

PF-05212384, also known as PKI-587 and Gedatolisib, is a dual phosphatidylinositol-3-kinase (PI3K) / mammalian target of rapamycin (mTOR) inhibitor. PKI-587 potently inhibited class I PI3Ks (IC50 vs PI3K-α = 0.4 nM), PI3K-α mutants, and mTOR. PF-05212384 inhibited growth of 50 diverse human tumor cell lines at IC50s <100 nM and has been in clinical trials in patients with advanced solid tumors. PF-05212384 has also been found to sensitize cells to radiation.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000114591
0000114592
0000074164
0000074165
045M4715V

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