PKI-402|cas:1173204-81-3|西域试剂

PKI-402,98.43%

产品编号：Bellancom-10683| CAS NO：1173204-81-3| 分子式：C₂₉H₃₄N₁₀O₃| 分子量：570.65

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-10683	￥1534.00	杭州北京（现货）
Bellancom-10683	￥2558.00	杭州北京（现货）
Bellancom-10683	￥7161.00	杭州北京（现货）
Bellancom-10683	￥12741.00	杭州北京（现货）

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PKI-402

产品介绍

PKI-402 是一种有效的 PI3K 和 mTOR 抑制剂，抑制 PI3Kα, mTOR, PI3Kβ, PI3Kδ 和 PI3Kγ，IC₅₀ 分别为 2, 3, 7, 14 和 16 nM。

生物活性

PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC₅₀=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).

体外研究

PKI-402 is an equipotent inhibitor of class I PI3K, including the E545K and H1047R PI3K-α mutants (IC₅₀=2, 3 and 3 nM for PI3Kα, PI3Kα-H1047R and PI3Kα-E545K, respectively). PKI-402 causes in vitro growth inhibition of human tumor cell lines derived from a diverse set of human tumor tissues, including breast, brain (glioma), pancreas, and non-small cell lung cancer (NSCLC) tissues. PKI-402 inhibits MDA-MB-361 [breast: Her2⁺ and PIK3CA mutant (E545K)], with an IC₅₀ of 6 nM. PKI-402 inhibits HCT116 (K-Ras and PIK3CA mutant) with an IC₅₀ of 33 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

PKI-402 displays antitumor activity (i.v. route) in breast [MDA-MB-361: Her2⁺ and PIK3CA (E545K)], glioma (U87MG and PTEN), and NSCLC (A549; K-Ras and STK11) xenograft models. PKI-402 causes regression in the MDA-MB-361 xenograft model. PKI-402 effect is most pronounced at 100 mg/kg (daily for 5 days, one round), which reduces initial tumor volume and prevents tumor re-growth for 70 days. In MDA-MB-361 tumor tissue, PKI-402 at 100 mg/kg (single dose) fully suppresses p-Akt at both the T308 and the S473 sites at 8 hours and induces cleaved PARP. At 24 hours, p-Akt suppression is still evident, as is cleaved PARP.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (8.76 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7524 mL	8.7619 mL	17.5239 mL
5 mM	0.3505 mL	1.7524 mL	3.5048 mL
10 mM	---	---	---

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式