PKI587 Inhibitor CAS No. 1197160-78-3

Cat. No.	Name	Size	Price
KI1058	PKI587	5 mg	$272
	PKI587	10 mg	$472
	PKI587	50 mg	$1170
	PKI587	200 mg	$3700

Chemical Characteristic

Product Name	PKI587
Synonyms	PF-05212384
CAS No.	1197160-78-3
Molecular Weight	615.32
Formula	C₃₂H₄₁N₉O₄
Chemical Name	N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea
Smiles	N(C(=O)Nc1ccc(cc1)c1nc(nc(n1)N1CCOCC1)N1CCOCC1)c1ccc(cc1)C(=O)N1CCC(CC1)N(C)C
Chemical Structure

Biological activities

PKI587 is a highly potent dual PI3K/mTOR kinase inhibitor. The IC50 of PKI587 is 0.4 nM against wild type PI3K-?. PKI587 inhibits mutant type PI3K-α^E545K and PI3K-α^H1047R with IC50 of 0.6 and 0.8 nM, respectively. In addition, PKI587 also blocks PI3K-β, PI3K-γ and PI3K-δ with IC50 of 6, 6 and 8 nM, respectively. In contrast, the IC50 of PKI587 is 1 nM against mTOR. PKI587 prevents growth of 50 diverse human tumor cell lines at IC50 values of less than 100 nM. PKI587 inhibits the growth of tumor cells MDA-MB-361, MDA-MB-468 and T47D with IC50 of 1, 6 and 2 nM, respectively. PKI587 suppresses the phosphorylation of PI3K/mTOR effectors (including Akt). PKI587 induces apoptosis in human tumor cell lines with elevated PI3K/mTOR signaling. PKI-587 at 25 mg/kg (single dose) suppresses p-Akt (T308 and S473) for up to 36 hours, with cPARP still evident at 18 hours. PKI587 inhibits EGF-stimulated AKT (ser473) activation.^[2] PKI587 suppresses Akt phosphorylation at S473.^[3] PKI587 prevents the proliferation of tumor in several models, including breast (MDA-MB-361, BT474), colon (HCT116), lung (H1975), and glioma (U87MG) xenograft models.^[1] PKI587 reveals excellent antitumor efficacy in both subcutaneous and orthotopic xenograft tumor models when administered intravenously.^[3]

Protocols

In vivo PKI587 is dissolved in 5% dextrose, water, pH 3.5.^[1]

References

[1] 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. [2] Gedaly R, et al. 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. [3] Venkatesan AM, 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.

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