貨號	規格	價格	上海	北京	武漢	南京
S81118-2mg	99.2%	￥297.50 S81118-2mg ￥297.50 現貨	8 8	-	-	-
S81118-5mg	99.2%	￥501.50 S81118-5mg ￥501.50 現貨	6 6	-	-	-
S81118-10mg	99.2%	￥977.50 S81118-10mg ￥977.50 現貨	7 7	-	-	-
S81118-25mg	99.2%	￥1615.00 S81118-25mg ￥1615.00 現貨	5 5	-	-	-
S81118-50mg	≥98%	￥2450.00 S81118-50mg ￥2450.00 2-3天	0 貨期：2-3天	-	-	-
S81118-100mg	≥98%	￥3900.00 S81118-100mg ￥3900.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.

產品描述：

Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.

靶點：

PI3Kα：39 nM (IC50)；PI3Kβ：383 nM (IC50)；PI3Kδ：36 nM (IC50)；PI3Kγ：23 nM (IC50)；Vps34：6974 nM (IC50)；DNA-PK：4750 nM (IC50);PI3K

體內研究：

The ability of Pilaralisib (XL147) to inhibit this endogenous phosphorylation of AKT, p70S6K, and S6 is examined following a single oral dose of 10, 30, 100, or 300 mg/kg. The tumors are harvested 4, 24, or 48 hours postdose and homogenized in lysis buffer. Tumor lysates from each animal (n=4) are then pooled for each group and analyzed for levels of total and phosphorylated AKT, p70S6K, and S6 by Western immunoblotting. Administration of Pilaralisib (XL147) causes a dose-dependent decrease in phosphorylation of AKT, p70S6K, and S6 in the tumors, reaching a maximum of 81% inhibition of AKT phosphorylation at 300 mg/kg at 4 hours. The dose-response relationships derived from the 4-hour time point predict 50% inhibition of AKT, p70S6K, and S6 phosphorylation at doses of approximately 100 mg/kg (pAKTT308), 54 mg/kg (pAKTS473), 71 mg/kg (p-p70S6K), and 103 mg/kg (pS6). The inhibition of AKT, p70S6K, and S6 phosphorylation in MCF7 tumors following a 100 mg/kg dose of Pilaralisib (XL147) is maximal at 4 hours, reaching 55% to 75%; however, the level of inhibition decreased to 8% to 45% by 24 hours, and only minimal or no inhibition was evident by 48 hours. Following a 300 mg/kg dose of Pilaralisib (XL147), inhibition is also maximal at 4 hours (65%-81%). However, in contrast with the 100 mg/kg dose, inhibition at 24 hours (51%-78%) is almost comparable with that seen at 4 hours, and partial inhibition (25%-51%) persisted through 48 hours

參考文獻：

1. Foster P, et al. The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models. Mol Cancer Ther. 2015 Apr;14(4):931-40.

溶解性：

DMSO : ≥ 100 mg/mL (184.84 mM)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.848 ml	9.242 ml	18.484 ml
5 mM	0.37 ml	1.848 ml	3.697 ml
10 mM	0.185 ml	0.924 ml	1.848 ml
50 mM	0.037 ml	0.185 ml	0.37 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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XL-147