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Eganelisib {[allProObj[0].p_purity_real_show]}

货号:A175847 同义名: IPI-549 Ambeed 开学季,买赠积分,赢豪礼

IPI-549 is a selective phosphoinositide-3-kinase (PI3K)-γ inhibitor with IC50 of 16 nM as an immuno-oncology clinical candidate.

Eganelisib 化学结构 CAS号:1693758-51-8
Eganelisib 化学结构
CAS号:1693758-51-8
Eganelisib 3D分子结构
CAS号:1693758-51-8
Eganelisib 化学结构 CAS号:1693758-51-8
Eganelisib 3D分子结构 CAS号:1693758-51-8
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Eganelisib 纯度/质量文件 产品仅供科研

货号:A175847 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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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。

Eganelisib 生物活性

靶点
  • p110γ

    PI3Kγ, IC50:16 nM

描述 PI3Ks are divided into three classes (I, II, and III) based on substrate specificity, sequence homology, and types of regulatory subunits. Class I PI3Ks are further divided into Class IA and Class IB. Class IB of PI3Ks containing the only member, PI3Kγ, is activated primarily by G-protein coupled receptors. The PI3Kγ isoform is mainly expressed in immune cells. Preclinical studies suggest that PI3Kγ inhibition in tumor-associated myeloid cells may be effective to prevent tumor growth. IPI-549 is a potent inhibitor of PI3Kγ (IC50 = 16 nM, measured by Promega ADP-Glo Max assay kit) with >100-fold selectivity over other lipid and protein kinases. IPI-549 shows excellent PI3Kγ potency (IC50 = 1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold) measured by cellular phospho-AKT inhibition assays in SKOV-3, 786-O, RAW 264.7, and RAJI cells. Also, IPI-549 inhibited PI3Kγ-dependent BMDM migration in a dose-dependent manner in vitro. 0.1 - 3 mg/kg oral treatment of IPI-549 significantly reduced neutrophil migration in a dose-dependent manner while a significant inhibition of PI3Kγ can be observed in the mouse air pouch model. IPI-549 is currently in Phase 1 clinical evaluation of advanced solid tumors[1].

Eganelisib 动物研究

Dose Mice: 15 mg/kg[2] (p.o.), 3 mg/kg[3] (i.p.)
Administration p.o, i.p.
Pharmacokinetics
Animal Mice[1] Rats[1] Dogs[1] Monkeys[1]
Dose 1 mg/kg 1 mg/kg 0.5 mg/kg 0.5 mg/kg
Administration i.v. i.v. i.v. i.v.
T1/2 3.2 h 4.4 h 6.7 h 4.3 h
Vss 0.8 L/kg 1.2 L/kg 1.3 L/kg 1.3 L/kg
CL 3.6 ml/min/kg 4.4 ml/min/kg 2.8 ml/min/kg 4.3 ml/min/kg
F 0.88 0.57 0.65 0.31

Eganelisib 参考文献

[1]Evans CA, Liu T, et al. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7.

[2]Kaneda MM, Messer KS, et al. PI3Kγ is a molecular switch that controls immune suppression. Nature. 2016 Nov 17;539(7629):437-442.

[3]De Vera AA, Gupta P, et al. Immuno-oncology agent IPI-549 is a modulator of P-glycoprotein (P-gp, MDR1, ABCB1)-mediated multidrug resistance (MDR) in cancer: In vitro and in vivo. Cancer Lett. 2019 Feb 1;442:91-103.

Eganelisib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.46mL

1.89mL

0.95mL

18.92mL

3.78mL

1.89mL

Eganelisib 技术信息

CAS号1693758-51-8
分子式C30H24N8O2
分子量 528.564
别名 IPI-549
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(47.3 mM),配合低频超声助溶,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
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