货号	规格	价格	上海	北京	珠海	重庆	武汉
V48104-1mg	≥98%	￥686.00 V48104-1mg ￥686.00 2-4周	0 货期：2-4周	-	-	-	-
V48104-5mg	≥98%	￥2400.00 V48104-5mg ￥2400.00 现货	9 9	-	-	-	-
V48104-10mg	≥98%	￥3900.00 V48104-10mg ￥3900.00 现货	6 6	-	-	-	-
V48104-25mg	≥98%	￥7900.00 V48104-25mg ￥7900.00 现货	3 3	-	-	-	-
V48104-50mg	≥98%	￥12700.00 V48104-50mg ￥12700.00 现货	3 3	-	-	-	-

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产品描述：

PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo.

靶点：

PI3Kα:8 nM (IC50); PI3Kβ:24 nM (IC50); PI3Kγ:74 nM (IC50); PI3Kδ:77 nM (IC50); mTOR:0.42 nM (IC50); E545K:14 nM (IC50); H1047R:11 nM (IC50)

体外研究：

PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors[1].
PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts[1].
PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) [1].

体内研究：

PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively.
PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC50=3 μM).

参考文献：

1. Venkatesan AM, et, al. PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5869-73.
2. Rehan M. A structural insight into the inhibitory mechanism of an orally active PI3K/mTOR dual inhibitor, PKI-179 using computational approaches. J Mol Graph Model. 2015 Nov;62:226-234.

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.047 ml	10.235 ml	20.469 ml
5 mM	0.409 ml	2.047 ml	4.094 ml
10 mM	0.205 ml	1.023 ml	2.047 ml
50 mM	0.041 ml	0.205 ml	0.409 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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