PKI587

PKI-587 (PF-05212384) is a highly potent dual PI3K/mTOR kinase inhibitor.PKI-587 (PF-05212384)potently inhibited class I PI3Ks (IC (50) vs. PI3K-α = 0.4 nmol/L), PI3K-α mutants, and mTOR.PKI-587 (PF-05212384) inhibited growth of 50 diverse human tumor cell lines at IC (50) values of less than 1nm.PKI-587 (PF-05212384) also inhibit 236 human protein kinases (IC50s >10 μM.Only wild type and mutant (V600E) B-Rafs were inhibited by PKI-587 at IC50 values of 10μM.


Cat. No.: EX-A028	Purity: >98%

	Chemical structure of PKI587

For research only, Do not use for Human!

Size	Unit Price (US$)	Stock
100mg	425	In-stock
250mg	700	In-stock
500mg	950	In-stock
1g	1450	In-stock
2g	2100	In-stock
5g	3900	In-stock

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Synonyms	Gedatolisib
CAS No.	1197160-78-3
Purity	>98%
Formula	C32H41N9O4
Mol Weight	615.7258
Appearance	solid powder
Solubility	Soluble in DMSO
Shelf Life	>3 years if stored properly
Storage	Powder -20℃ 3 years; In solvent -20℃ 1 month;
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[1]. Gedaly R, Angulo P, Hundley J, Daily MF, Chen C, Evers BM. PKI-587 and sorafenib targeting PI3K/AKT/mTOR and Ras/Raf/MAPK pathways synergistically inhibit HCC cell proliferation. J Surg Res. 2012;176(2):542-548. doi:10.1016/j.jss.2011.10.045 [1]. Mallon R, Feldberg LR, Lucas J, et al. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin Cancer Res. 2011;17(10):3193-3203. doi:10.1158/1078-0432.CCR-10-1694 [1]. Venkatesan AM, Dehnhardt CM, Delos Santos E, et al. Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J Med Chem. 2010;53(6):2636-2645. doi:10.1021/jm901830p
CoA	CoA of PKI587

Smiles:	CN(C)C1CCN(CC1)C(=O)C1=CC=C(NC(=O)NC2=CC=C(C=C2)C2=NC(=NC(=N2)N2CCOCC2)N2CCOCC2)C=C1


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