Gedatolisib - CAS:1197160-78-3

您当前的位置：

Gedatolisib (Synonyms:PKI-587; PF-05212384)

目录号 : KM2709 CAS No. : 1197160-78-3 纯度 : 98%

Data Sheet SDS 产品使用指南

Gedatolisib (PKI-587) 是一种高效的双重 PI3Kα，PI3Kγ 和 mTOR 抑制剂, IC₅₀ 分别为 0.4 nM，5.4 nM 和 1.6 nM。Gedatolisib 在 mTOR 复合物 mTORC1 和 mTORC2 中同样有效。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock
200mg	询价	In-stock
500mg	询价	In-stock

查看所有商品（1）

加入购物车大包装询价

Other Forms of Rapamycin:

Polyvinyl alcohol (Mw 13000-23000, 98% hydrolyzed) In-stock
Opitor-0 In-stock
Ginkgolide B In-stock
Isoginkgetin In-stock
Ginkgolic acid C17:1 In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC₅₀s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2.

IC₅₀&Target

PI3Kα

0.4 nM (IC₅₀)

PI3Kα-H1047R

0.6 nM (IC₅₀)

PI3Kα-E545K

0.6 nM (IC₅₀)

PI3Kγ

5.4 nM (IC₅₀)

PI3Kβ

6 nM (IC₅₀)

PI3Kδ

6 nM (IC₅₀)

mTOR

1.6 nM (IC₅₀)

mTORC1

mTORC2

体外研究

Gedatolisib (PKI-587) shows good potency in cell growth inhibition assays using MDA-361 and PC3-MM2 cell lines with IC₅₀s of 4.0 and 13.1 nM, respectively.
Gedatolisib shows potent suppression of phosphorylation of PI3K/mTOR signaling pathway proteins in MDA-361 tumor cells. Gedatolisib (0.03-3 μM; 4 hours) prevents the phosphorylation of Akt at Thr 308 and induces cleaved PARP at 30 nM.

Western Blot Analysis

Cell Line:	MDA-361 tumor cells
Concentration:	0.03, 0.1, 0.3, 1, and 3 μM
Incubation Time:	4 hours
Result:	Prevented the phosphorylation of Akt (pAkt) at threonine 308 (T308; IC₅₀=8 nM).

体内研究

Gedatolisib (PKI-587; administered i.v. at 20 mg/kg on days 1, 5, 9) exhibits potent antitumor efficacy against MDA-361 tumors in mice.
Gedatolisib exhibits terminal elimination half-life (T_1/2 14.4 h) due to high plasma clearance (7 mL/min/kg) combined with large volumes of distribution (7.2 L/kg respectively) following i.v. administration (25 mg/kg) female nude mice.

Animal Model:	Female nude mice bearing MDA-361 xenograft model.
Dosage:	20 mg/kg
Administration:	Administered i.v. at 20 mg/kg on an intermittent regimen (days 1, 5, 9).
Result:	Caused regression of large staged (~900 mm) tumors. The minimum efficacious dose (MED) was determined to be 3 mg/kg against MDA-361 tumors and maximum tolerated single dose (MTD) was determined to be 30 mg/kg.

分子式

C₃₂H₄₁N₉O₄

分子量

615.73

CAS号

1197160-78-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vitro:

DMSO : 4 mg/mL (6.50 mM; Need warming)

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	1.6241 mL	8.1204 mL	16.2409 mL
5 mM	0.3248 mL	1.6241 mL	3.2482 mL
10 mM	---	---	---

科研文献

纯度： 98%

Data Sheet

SDS

产品使用指南

暂无相关参考文献

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 4 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器