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PKI-402

Chemical Structure : PKI-402

CAS No.: 1173204-81-3

PKI-402 (PKI 402;PKI402)

Catalog No.: PC-42695Not For Human Use, Lab Use Only.

PKI-402 is a potent dual PI3K/mTOR inhibitor with IC50 of 1/7/16/14/1.7 nM for PI3Kα/β/γ/δ/mTOR respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PKI-402 is a potent dual PI3K/mTOR inhibitor with IC50 of 1/7/16/14/1.7 nM for PI3Kα/β/γ/δ/mTOR respectively.
PKI-402 shows excellent suppression of Akt T308 phosphorylation (IC50=5 nM), and excellent inhibition of cell proliferation in several human cancer cell lines.
PKI-402 shows excellent in vivo efficacy in various human cancer xenografts, good physical properties and PK parameters.

Physicochemical Properties

M.Wt 570.6454
Formula C29H34N10O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: < 1 mg/mL

Chemical Name/SMILES

Urea, N-[4-[3-ethyl-7-(4-morpholinyl)-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-yl]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-

References

1. Dehnhardt CM, et al. J Med Chem. 2010 Jan 28;53(2):798-810.

2. Mallon R, et al. Mol Cancer Ther. 2010 Apr;9(4):976-84.

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