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PKI-402
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PKI-402图片
CAS NO:1173204-81-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
PKI-402 是一种有效的PI3KmTOR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 ofPI3K, including PI3K-α mutants, andmTOR(IC50=2, 3, 7,14 and 16 nM forPI3Kα,mTOR,PI3Kβ,PI3Kδand PI3Kγ).

IC50& Target[1]

PI3Kα

2 nM (IC50)

PI3Kα-H1047R

3 nM (IC50)

PI3Kα-E545K

3 nM (IC50)

PI3Kβ

7 nM (IC50)

PI3Kδ

14 nM (IC50)

PI3Kγ

16 nM (IC50)

mTOR

3 nM (IC50)

体外研究
(In Vitro)

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+andPIK3CAmutant (E545K)], with an IC50of 6 nM. PKI-402 inhibits HCT116 (K-Ras andPIK3CAmutant) with an IC50of 33 nM[1].

体内研究
(In Vivo)

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[1].

分子量

570.65

性状

Solid

Formula

C29H34N10O3

CAS 号

1173204-81-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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 mg5 mg10 mg
1 mM1.7524 mL8.7619 mL17.5239 mL
5 mM0.3505 mL1.7524 mL3.5048 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。