GSK2636771 | PI3K | AmBeed-信号通路专用抑制剂

首页 / / / PI3K / GSK2636771

GSK2636771 {[allProObj[0].p_purity_real_show]}

货号：A169634

GSK2636771 is a potent, selective and orally bioavailable PI3Kβ inhibitor. It has been used in trials studying the treatment of CANCER, LYMPHOMA, Solid Neoplasm, Recurrent Solid Neoplasm, and Advanced Malignant Neoplasm, among others.

GSK2636771 化学结构
CAS号：1372540-25-4

GSK2636771 3D分子结构
CAS号：1372540-25-4

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]}	现货	咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

GSK2636771 纯度/质量文件产品仅供科研

货号：A169634 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

PI3K 亚型比较

产品名称	C2β ↓ ↑	p110α ↓ ↑	p110β ↓ ↑	p110γ ↓ ↑	p110δ ↓ ↑	PI3K ↓ ↑	Vps34 ↓ ↑	其他靶点	纯度
A66	+ C2β, IC50: 462 nM	++ p110α, IC50: 32 nM							{[allProObj[0].p_purity_real_show]}
Taselisib	+ C2β, IC50: 292 nM	++++ PI3Kα, Ki: 0.29 nM	+++ PI3Kβ, Ki: 9.1 nM	++++ PI3Kγ, Ki: 0.97 nM	++++ PI3Kδ, Ki: 0.12 nM		+ hVps34, IC50: 374 nM		{[allProObj[0].p_purity_real_show]}
Gedatolisib		++++ PI3Kα, IC50: 0.4 nM		+++ PI3Kγ, IC50: 5.4 nM				mTOR	{[allProObj[0].p_purity_real_show]}
HS-173		++++ PI3Kα , IC50: 0.8 nM							{[allProObj[0].p_purity_real_show]}
Serabelisib		+++ PI3Kα, IC50: 21 nM							{[allProObj[0].p_purity_real_show]}
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	{[allProObj[0].p_purity_real_show]}
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	{[allProObj[0].p_purity_real_show]}
AS-252424		+ PI3Kα, IC50: 935 nM		++ PI3Kγ, IC50: 33 nM					{[allProObj[0].p_purity_real_show]}
Alpelisib		+++ PI3Kα, IC50: 5 nM							{[allProObj[0].p_purity_real_show]}
AS-604850		+ PI3Kα, IC50: 4.5 μM		+ PI3Kγ, IC50: 0.25 μM					{[allProObj[0].p_purity_real_show]}
SF2523		++ PI3Kα, IC50: 34 nM		++ PI3Kγ, IC50: 158 nM				DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
Inavolisib		++++ PI3K alpha, IC50: 0.038 nM							{[allProObj[0].p_purity_real_show]}
Bimiralisib		++++ PI3Kα, Kd: 1.5 nM	+++ PI3Kβ, Kd: 11 nM	++ PI3Kγ, Kd: 25 nM	++ PI3Kδ, Kd: 25 nM			mTOR	{[allProObj[0].p_purity_real_show]}
GSK1059615		++++ PI3Kα, IC50: 0.4 nM	++++ PI3Kβ, IC50: 0.6 nM	+++ PI3Kγ, IC50: 5 nM	++++ PI3Kδ, IC50: 2 nM			mTOR	{[allProObj[0].p_purity_real_show]}
GSK2636771			✔						{[allProObj[0].p_purity_real_show]}
Fimepinostat		+++ PI3Kα, IC50: 19 nM	++ PI3Kβ, IC50: 54 nM		++ PI3Kδ, IC50: 39 nM				{[allProObj[0].p_purity_real_show]}
VS-5584		++++ PI3Kα, IC50: 2.6 nM	+++ PI3Kβ, IC50: 21 nM	++++ PI3Kγ, IC50: 3.0 nM	++++ PI3Kδ, IC50: 2.7 nM			mTOR	{[allProObj[0].p_purity_real_show]}
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				{[allProObj[0].p_purity_real_show]}
PI-103		++++ p110α, IC50: 2 nM	++++ p110β, IC50: 3 nM	+++ p110γ, IC50: 15 nM	++++ p110δ, IC50: 3 nM			DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
PI-3065			+ p110β, IC50: 1078 nM		+++ p110δ, IC50: 15 nM				{[allProObj[0].p_purity_real_show]}
Voxtalisib		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
AZD-8835		+++ PI3Kα, IC50: 6.2 nM	+ PI3Kβ, IC50: 431 nM	++ PI3Kγ, IC50: 90 nM	+++ PI3Kδ, IC50: 5.7 nM				{[allProObj[0].p_purity_real_show]}
Pilaralisib analogue		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 36 nM	+++ PI3Kγ, IC50: 23 nM	++ PI3Kδ, IC50: 36 nM				{[allProObj[0].p_purity_real_show]}
ZSTK474		+++ PI3Kα, IC50: 16 nM	++ PI3Kβ, IC50: 44 nM	++ PI3Kγ, IC50: 49 nM	+++ PI3Kδ, IC50: 4.6 nM	++ PI3K, IC50: 37 nM			{[allProObj[0].p_purity_real_show]}
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				{[allProObj[0].p_purity_real_show]}
TGX-221			+++ p110β, IC50: 5 nM		++ p110δ, IC50: 0.1 μM				{[allProObj[0].p_purity_real_show]}
PF-04691502		++++ PI3Kα, Ki: 1.8 nM	++++ PI3Kβ, Ki: 2.1 nM	++++ PI3Kγ, Ki: 1.9 nM	++++ PI3Kδ, Ki: 1.6 nM			mTOR	{[allProObj[0].p_purity_real_show]}
GDC-0084		++++ PI3Kα, Ki app: 2 nM	++ PI3Kβ, Ki app: 46 nM	+++ PI3Kγ, Ki app: 10 nM	++++ PI3Kδ, Ki app: 3 nM			mTOR	{[allProObj[0].p_purity_real_show]}
Buparlisib		++ p110α, IC50: 52 nM	+ p110β, IC50: 166 nM	+ p110γ, IC50: 262 nM	++ p110δ, IC50: 116 nM		+ Vps34, IC50: 2.4 μM	mTOR	{[allProObj[0].p_purity_real_show]}
LY294002		+ p110α, IC50: 0.5 μM	+ p110β, IC50: 0.97 μM		+ p110δ, IC50: 0.57 μM			DNA-PK	{[allProObj[0].p_purity_real_show]}
AZD 6482		+ PI3Kα, IC50: 870 nM	+++ PI3Kβ, IC50: 10 nM		++ PI3Kδ, IC50: 80 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Pictilisib		++++ p110α, IC50: 3 nM	++ p110β, IC50: 33 nM	++ p110γ, IC50: 75 nM	++++ p110δ, IC50: 3 nM			mTOR	{[allProObj[0].p_purity_real_show]}
PKI-402		++++ PI3Kα, IC50: 2 nM	+++ PI3Kβ, IC50: 7 nM	+++ PI3Kγ, IC50: 16 nM	+++ PI3Kδ, IC50: 14 nM			mTOR	{[allProObj[0].p_purity_real_show]}
Copanlisib		++++ PI3Kα, IC50: 0.5 nM	++++ PI3Kβ, IC50: 3.7 nM	+++ PI3Kγ, IC50: 6.4 nM	++++ PI3Kδ, IC50: 0.7 nM				{[allProObj[0].p_purity_real_show]}
Omipalisib		++++ p110α, Ki: 0.019 nM	++++ p110β, Ki: 0.13 nM	++++ p110γ, Ki: 0.06 nM	++++ p110δ, Ki: 0.024 nM				{[allProObj[0].p_purity_real_show]}
Izorlisib		+++ PI3Kα, IC50: 14 nM	++ PI3Kβ, IC50: 0.12 μM	++ PI3Kγ, IC50: 36 nM	+ PI3Kδ, IC50: 0.50 μM				{[allProObj[0].p_purity_real_show]}
AZD8186		++ PI3Kα, IC50: 35 nM	++++ PI3Kβ, IC50: 4 nM		+++ PI3Kδ, IC50: 12 nM				{[allProObj[0].p_purity_real_show]}
KU-0060648		++++ PI3Kα, IC50: 4 nM	++++ PI3Kβ, IC50: 0.5 nM	+ PI3Kγ, IC50: 0.59 μM	++++ PI3Kδ, IC50: 0.1 nM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	{[allProObj[0].p_purity_real_show]}
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					{[allProObj[0].p_purity_real_show]}
BGT226 maleate		++++ PI3Kα, IC50: 4 nM	++ PI3Kβ, IC50: 63 nM	++ PI3Kγ, IC50: 38 nM				mTOR	{[allProObj[0].p_purity_real_show]}
TG 100713		++ PI3Kα, IC50: 165 nM	+ PI3Kβ, IC50: 215 nM	++ PI3Kγ, IC50: 50 nM	+++ PI3Kδ, IC50: 24 nM				{[allProObj[0].p_purity_real_show]}
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				{[allProObj[0].p_purity_real_show]}
PIK-90		+++ PI3Kα, IC50: 11 nM	+ PI3Kβ, IC50: 350 nM	+++ PI3Kγ, IC50: 18 nM	++ PI3Kδ, IC50: 58 nM				{[allProObj[0].p_purity_real_show]}
PIK-294			+ p110β, IC50: 490 nM	++ p110γ, IC50: 160 nM	+++ p110δ, IC50: 10 nM				{[allProObj[0].p_purity_real_show]}
Duvelisib			++++ PI3Kβ, Ki: 1564 pM	++ PI3Kγ, Ki: 243 pM	++++ PI3Kδ, Ki: 23 pM				{[allProObj[0].p_purity_real_show]}
GDC-0326		++++ PI3Kα, Ki: 0.2 nM	++ PI3Kβ, Ki: 26.6 nM	+++ PI3Kγ, Ki: 10.2 nM	++++ PI3Kδ, Ki: 4 nM				{[allProObj[0].p_purity_real_show]}
Quercetin Dihydrate			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM				{[allProObj[0].p_purity_real_show]}
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Sirtuin,PKC,Src	{[allProObj[0].p_purity_real_show]}
Leniolisib		+ PI3Kα, IC50: 0.244 μM	+ PI3Kβ, IC50: 0.424 μM	+ PI3Kγ, IC50: 2.23 μM	+++ PI3Kδ, IC50: 0.011 μM			DNA-PK	{[allProObj[0].p_purity_real_show]}
PIK-108			✔						{[allProObj[0].p_purity_real_show]}
Eganelisib				+++ PI3Kγ, IC50: 16 nM					{[allProObj[0].p_purity_real_show]}
CAY10505				✔					{[allProObj[0].p_purity_real_show]}
IPI-3063					++++ p110δ, IC50: 2.5 nM				{[allProObj[0].p_purity_real_show]}
Nemiralisib					++++ PI3Kδ, pKi: 9.9				{[allProObj[0].p_purity_real_show]}
PF-4989216		++++ p110α, IC50: 2 nM		++ p110γ, IC50: 65 nM	++++ p110δ, IC50: 1 nM				{[allProObj[0].p_purity_real_show]}
PIK-75 HCl		+++ p110α, IC50: 5.8 nM		++ p110γ, IC50: 76 nM	+ p110δ, IC50: 0.51 μM			DNA-PK	{[allProObj[0].p_purity_real_show]}
Tenalisib				++ PI3Kγ, IC50: 33.2 nM	++ PI3Kδ, IC50: 24.5 nM				{[allProObj[0].p_purity_real_show]}
Acalisib					+++ p110δ, IC50: 14 nM				{[allProObj[0].p_purity_real_show]}
Umbralisib					+++ PI3Kδ, IC50: 22.2 nM				{[allProObj[0].p_purity_real_show]}
AMG319				+ PI3Kγ, IC50: 850 nM	+++ PI3Kδ, IC50: 18 nM				{[allProObj[0].p_purity_real_show]}
IC-87114				+ PI3Kγ, IC50: 29 μM	+ PI3Kδ, IC50: 0.5 μM				{[allProObj[0].p_purity_real_show]}
Idelalisib				++ p110γ, IC50: 89 nM	++++ p110δ, IC50: 2.5 nM				{[allProObj[0].p_purity_real_show]}
PIK-293				+ p110γ, IC50: 10 μM	+ p110δ, IC50: 0.24 μM				{[allProObj[0].p_purity_real_show]}
Vps34-PIK-III					+ PI3Kδ, IC50: 1.2μM		+++ Vps34, IC50: 0.018μM		{[allProObj[0].p_purity_real_show]}
GSK2292767					✔				{[allProObj[0].p_purity_real_show]}
Seletalisib				+ PI3Kγ, IC50: 282 nM	+++ PI3Kδ, IC50: 12 nM				{[allProObj[0].p_purity_real_show]}
P110δ-IN-1					++++ P110δ, IC50: 0.6 nM				{[allProObj[0].p_purity_real_show]}
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				{[allProObj[0].p_purity_real_show]}
SRX3207		+ PI3K alpha, IC50: 244 nM		+ PI3K gamma, IC50: 9790 nM	+ PI3K delta, IC50: 388 nM			Syk	{[allProObj[0].p_purity_real_show]}
Parsaclisib HCl					++++ PI3Kδ, IC50: 1 nM				{[allProObj[0].p_purity_real_show]}
IHMT-PI3Kδ-372					+++ PI3Kδ, IC50: 14 nM				{[allProObj[0].p_purity_real_show]}
Trigonelline						✔		Akt	{[allProObj[0].p_purity_real_show]}
Wortmannin						++++ PI3K, IC50: 3 nM		MLCK,DNA-PK	{[allProObj[0].p_purity_real_show]}
Samotolisib						✔		DNA-PK	{[allProObj[0].p_purity_real_show]}
GNE-317						✔			{[allProObj[0].p_purity_real_show]}
Oroxin B						✔		PTEN,Akt	{[allProObj[0].p_purity_real_show]}
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	{[allProObj[0].p_purity_real_show]}
Deguelin						✔		Akt	{[allProObj[0].p_purity_real_show]}
Ailanthone						✔		Akt,ATM/ATR,CDK	{[allProObj[0].p_purity_real_show]}
Resibufogenin						✔		ROS	{[allProObj[0].p_purity_real_show]}
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	{[allProObj[0].p_purity_real_show]}
Cinobufagine						✔		Akt	{[allProObj[0].p_purity_real_show]}
α-Linolenic acid						✔			{[allProObj[0].p_purity_real_show]}
MTX-211						✔		EGFR	{[allProObj[0].p_purity_real_show]}
PI3K/mTOR Inhibitor-2						++++ PI3K, IC50: 3.4 nM		mTOR	{[allProObj[0].p_purity_real_show]}
SPP-86						✔			{[allProObj[0].p_purity_real_show]}
(E)-Akt inhibitor-IV						✔			{[allProObj[0].p_purity_real_show]}
Vps34-IN-1							++ Vps34, IC50: 25 nM		{[allProObj[0].p_purity_real_show]}
SAR405							++++ Vps34, IC50: 1.2 nM		{[allProObj[0].p_purity_real_show]}
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	{[allProObj[0].p_purity_real_show]}
Vps34-IN-4							+++ VPS34, IC50: 15 nM		{[allProObj[0].p_purity_real_show]}
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

GSK2636771 生物活性

靶点

p110β

描述

The PI3K/protein kinase B (AKT) pathway is commonly activated in several tumor types. Selective targeting of p110β could result in successful pathway inhibition while avoiding the on- and off-target effects of pan-PI3K inhibitors. GSK2636771 is a potent, orally bioavailable, adenosine triphosphate-competitive, selective inhibitor of PI3Kβ with IC₅₀s of 3.5 nM, 20.49 nM, 40.53 nM for p110α p110β and p110γ, respectively^[3]. In a vivo study, female nude mice with tumor xenografts were treated with vehicle or GSK2636771 at 1, 3, 10, or 30 mg/kg by oral gavage for 21 days and GSK2636771 resulted in tumor growth inhibition. In a cell study, C4-2B cells and its MDV3100-resistant subline was pretreated with GSK2636771 range from 1-100μM in 30mins. The result showed that treatment with GSK2636771 significantly increased G0/G1 population accompanied with a large reduction of S-phase cells not only in C4-2B cells but also in C4-2B/MDV-R cells, although the extent of G1/G0 phase arrest in MDV-R cells was less than that in the parental C4-2B cells^[4].

GSK2636771 参考文献

[1]Leroy C, Ramos P, et al. Activation of IGF1R/p110β/AKT/mTOR confers resistance to α-specific PI3K inhibition. Breast Cancer Res. 2016 Apr 5;18(1):41.

[2]Weigelt B, Warne PH, et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3533-44.

[3]Mateo J, Ganji G, Lemech C, Burris HA, Han SW, Swales K, Decordova S, DeYoung MP, Smith DA, Kalyana-Sundaram S, Wu J, Motwani M, Kumar R, Tolson JM, Rha SY, Chung HC, Eder JP, Sharma S, Bang YJ, Infante JR, Yan L, de Bono JS, Arkenau HT. A First-Time-in-Human Study of GSK2636771, a Phosphoinositide 3 Kinase Beta-Selective Inhibitor, in Patients with Advanced Solid Tumors. Clin Cancer Res. 2017 Oct 1;23(19):5981-5992. doi: 10.1158/1078-0432.CCR-17-0725. Epub 2017 Jun 23. PMID: 28645941.

[4]He C, Duan S, Dong L, Wang Y, Hu Q, Liu C, Forrest ML, Holzbeierlein JM, Han S, Li B. Characterization of a novel p110β-specific inhibitor BL140 that overcomes MDV3100-resistance in castration-resistant prostate cancer cells. Prostate. 2017 Aug;77(11):1187-1198. doi: 10.1002/pros.23377. Epub 2017 Jun 20. PMID: 28631436; PMCID: PMC5527967.

GSK2636771 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.54mL

2.31mL

1.15mL

23.07mL

4.61mL

2.31mL

GSK2636771 技术信息

CAS号	1372540-25-4
分子式	C₂₂H₂₂F₃N₃O₃
分子量	433.424

别名
运输	蓝冰

存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 16 mg/mL(36.92 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

GSK2636771 {[allProObj[0].p_purity_real_show]}

GSK2636771 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

GSK2636771 质控信息

GSK2636771 生物活性

GSK2636771 参考文献

GSK2636771 实验方案

GSK2636771 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

GSK2636771 {[allProObj[0].p_purity_real_show]}

GSK2636771 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GSK2636771 质控信息

GSK2636771 生物活性

GSK2636771 参考文献

GSK2636771 实验方案

GSK2636771 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

GSK2636771 纯度/质量文件产品仅供科研