Bimiralisib | PI3K Inhibitor | AmBeed-信号通路专用抑制剂

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Bimiralisib {[allProObj[0].p_purity_real_show]}

货号：A719240 同义名： PQR309;PI3K-IN-2

PQR309 is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively.

Bimiralisib 化学结构
CAS号：1225037-39-7

Bimiralisib 3D分子结构
CAS号：1225037-39-7

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Bimiralisib 纯度/质量文件产品仅供科研

货号：A719240 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				mTOR,DNA-PK	{[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			mTOR,DNA-PK	{[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			mTOR,DNA-PK	{[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			mTOR,DNA-PK	{[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			PKC,Sirtuin,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		DNA-PK,MLCK	{[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						✔		Akt,PTEN	{[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,CDK,ATM/ATR	{[allProObj[0].p_purity_real_show]}
Resibufogenin						✔		ROS	{[allProObj[0].p_purity_real_show]}
KU-57788						+ PI3K, IC50: 5 μM		mTOR,DNA-PK	{[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。

Bimiralisib 生物活性

靶点	p110γ PI3Kγ, Kd:25 nM p110β PI3Kβ, Kd:11 nM p110α PI3Kα, Kd:1.5 nM p110δ PI3Kδ, Kd:25 nM
描述	Phosphoinositide 3-kinases (PI3Ks) are lipid kinases that play a central role in the control of cancer cell growth, proliferation, and metastasis. PI3K is deregulated in a wide variety of human tumors and triggers activation of protein kinase B (PKB/Akt) and mammalian target of rapamycin (mTOR). PQR309, a potent pan-class I PI3K inhibitor, targets mTOR kinase in a balanced fashion at higher concentrations. And it displays a mTOR/PI3Kα K_i selectivity ratio in the range of 3–8^[1]. In 49 lymphoma cell lines, PQR309 showed in vitro activity in most of them tested with a median IC₅₀ value of 233 nmol/L (95% CI, 174–324 nmol/L). The arrest in proliferation was mainly due to cell cycle arrest with a block in G₁ rather than to apoptosis, limited to only 2/7 cell lines^[2]. The half-life of 5–8 h and an AUC_0.25–12 of around 14000 h·ng/mL contributed to an excellent oral bioavailability of PQR309 (>50%). Male Beagle dogs, exposed to PQR309 at 10 mg/kg po, showed maximal drug plasma concentrations C_max of 583 ng/mL (approximately 1.5 μM) after 60–90 min and a half-life of >7 h, which results in drug levels of approximately 0.38 μM (150 ng/mL) after 24 h. The oral bioavailability of PQR309 in male Beagle dogs was estimated to be 23%^[1].
作用机制	One morpholine of PQR309 forms a hydrogen bridge with the backbone amide of Val882, a well-known and crucial interaction^[1].

Bimiralisib 参考文献

[1]5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology

[2]PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy

Bimiralisib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.15mL

2.43mL

1.22mL

24.31mL

4.86mL

2.43mL

Bimiralisib 技术信息

CAS号	1225037-39-7
分子式	C₁₇H₂₀F₃N₇O₂
分子量	411.382

别名	PQR309;PI3K-IN-2
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(121.54 mM)，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

Bimiralisib {[allProObj[0].p_purity_real_show]}

Bimiralisib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Bimiralisib 质控信息

Bimiralisib 生物活性

Bimiralisib 参考文献

Bimiralisib 实验方案

Bimiralisib 技术信息

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p110γ	PI3Kγ, Kd:25 nM
p110β	PI3Kβ, Kd:11 nM
p110α	PI3Kα, Kd:1.5 nM
p110δ	PI3Kδ, Kd:25 nM

Bimiralisib {[allProObj[0].p_purity_real_show]}

Bimiralisib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Bimiralisib 质控信息

Bimiralisib 生物活性

Bimiralisib 参考文献

Bimiralisib 实验方案

Bimiralisib 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

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Bimiralisib 纯度/质量文件产品仅供科研