PKI-402 Inhibitor CAS No. 1173204-81-3

Cat. No.	Name	Size	Price
KI1138	PKI-402	5 mg	$408
	PKI-402	10 mg	$770
	PKI-402	50 mg	$2200
	PKI-402	200 mg	$7040

Chemical Characteristic

Product Name	PKI-402
CAS No.	1173204-81-3
Molecular Weight	570.65
Formula	C₂₉H₃₄N₁₀O₃
Chemical Name	1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea
Smiles	N(C(=O)Nc1ccc(cc1)C(=O)N1CCN(CC1)C)c1ccc(cc1)c1nc2c(c(n1)N1CCOCC1)nnn2CC
Chemical Structure

Biological activities

PKI-402 is a selective, reversible and ATP-competitive inhibitor of class I phosphatidylinositol 3-kinases (PI3K). PKI-402 inhibits class I PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ with IC50 of 2, 7, 14 and 16 nM, respectively. PKI-402 also inhibits PI3K-α mutants E545K and H1047R, and mTOR with IC50 of 3, 3 and 3 nM, respectively. ^[1] In vitro, PKI-402 inhibits breast cell lines MDA-MB-361, MDA-MB-468, T47D and BT474 with IC50 of 6, 9, 13 and 26 nM, respectively. PKI-402 inhibits the growth of human tumor cell lines derived from breast, brain (glioma), pancreas, and non??mall cell lung cancer tissue. PKI-402 suppresses phosphorylation of PI3K and mTOR effector proteins. In vivo, PKI-587 inhibits tumor growth in breast (MDA-MB-361, BT474), colon (HCT116), lung (H1975), and glioma (U87MG) xenograft models. ^[2]

References

[1] Mallon R, et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010, 9(4): 976-984. [2] Mallon R, et al. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin Cancer Res. 2011, 17(10): 3193-3203.

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