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PIK-294 {[allProObj[0].p_purity_real_show]}

货号:A326767

PIK-294 is a potent and selective p110δ inhibitor with IC50 of 10 nM while 10,000/490/160 nM for p110α/β/γ.

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PIK-294 化学结构 CAS号:900185-02-6
PIK-294 化学结构
CAS号:900185-02-6
PIK-294 3D分子结构
CAS号:900185-02-6
PIK-294 化学结构 CAS号:900185-02-6
PIK-294 3D分子结构 CAS号:900185-02-6
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PIK-294 纯度/质量文件 产品仅供科研

货号:A326767 标准纯度: {[allProObj[0].p_purity_real_show]}
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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

99%+
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

99%+
Gedatolisib ++++

PI3Kα, IC50: 0.4 nM

+++

PI3Kγ, IC50: 5.4 nM

mTOR 98%
HS-173 ++++

PI3Kα , IC50: 0.8 nM

99%+
Serabelisib +++

PI3Kα, IC50: 21 nM

99%+
GNE-477 ++++

PI3Kα, IC50: 4 nM

mTOR 98%
YM-201636 +

p110α, IC50: 3.3 μM

PIKfyve 98%
AS-252424 +

PI3Kα, IC50: 935 nM

++

PI3Kγ, IC50: 33 nM

99%
Alpelisib +++

PI3Kα, IC50: 5 nM

99%+
AS-604850 +

PI3Kα, IC50: 4.5 μM

+

PI3Kγ, IC50: 0.25 μM

98+%
SF2523 ++

PI3Kα, IC50: 34 nM

++

PI3Kγ, IC50: 158 nM

mTOR,DNA-PK 99%+
Inavolisib ++++

PI3K alpha, IC50: 0.038 nM

99%+
Bimiralisib ++++

PI3Kα, Kd: 1.5 nM

+++

PI3Kβ, Kd: 11 nM

++

PI3Kγ, Kd: 25 nM

++

PI3Kδ, Kd: 25 nM

mTOR 99%+
GSK1059615 ++++

PI3Kα, IC50: 0.4 nM

++++

PI3Kβ, IC50: 0.6 nM

+++

PI3Kγ, IC50: 5 nM

++++

PI3Kδ, IC50: 2 nM

mTOR 98%
GSK2636771 98%
Fimepinostat +++

PI3Kα, IC50: 19 nM

++

PI3Kβ, IC50: 54 nM

++

PI3Kδ, IC50: 39 nM

99%+
VS-5584 ++++

PI3Kα, IC50: 2.6 nM

+++

PI3Kβ, IC50: 21 nM

++++

PI3Kγ, IC50: 3.0 nM

++++

PI3Kδ, IC50: 2.7 nM

mTOR 99%
Dactolisib ++++

p110α1, IC50: 4 nM

++

p110β, IC50: 75 nM

+++

p110γ, IC50: 5 nM

+++

p110δ, IC50: 7 nM

98+%
PI-103 ++++

p110α, IC50: 2 nM

++++

p110β, IC50: 3 nM

+++

p110γ, IC50: 15 nM

++++

p110δ, IC50: 3 nM

mTOR,DNA-PK 99%+
PI-3065 +

p110β, IC50: 1078 nM

+++

p110δ, IC50: 15 nM

99%+
Voxtalisib ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 113 nM

+++

PI3Kγ, IC50: 9 nM

++

PI3Kδ, IC50: 43 nM

mTOR,DNA-PK 99%+
AZD-8835 +++

PI3Kα, IC50: 6.2 nM

+

PI3Kβ, IC50: 431 nM

++

PI3Kγ, IC50: 90 nM

+++

PI3Kδ, IC50: 5.7 nM

98%
Pilaralisib analogue ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 36 nM

+++

PI3Kγ, IC50: 23 nM

++

PI3Kδ, IC50: 36 nM

99%+
ZSTK474 +++

PI3Kα, IC50: 16 nM

++

PI3Kβ, IC50: 44 nM

++

PI3Kγ, IC50: 49 nM

+++

PI3Kδ, IC50: 4.6 nM

++

PI3K, IC50: 37 nM

98%
AS-605240 ++

PI3Kα, IC50: 60 nM

+

PI3Kβ, IC50: 270 nM

+++

PI3Kγ, IC50: 8 nM

+

PI3Kδ, IC50: 300 nM

98%
TGX-221 +++

p110β, IC50: 5 nM

++

p110δ, IC50: 0.1 μM

99%+
PF-04691502 ++++

PI3Kα, Ki: 1.8 nM

++++

PI3Kβ, Ki: 2.1 nM

++++

PI3Kγ, Ki: 1.9 nM

++++

PI3Kδ, Ki: 1.6 nM

mTOR 98+%
GDC-0084 ++++

PI3Kα, Ki app: 2 nM

++

PI3Kβ, Ki app: 46 nM

+++

PI3Kγ, Ki app: 10 nM

++++

PI3Kδ, Ki app: 3 nM

mTOR 99%+
Buparlisib ++

p110α, IC50: 52 nM

+

p110β, IC50: 166 nM

+

p110γ, IC50: 262 nM

++

p110δ, IC50: 116 nM

+

Vps34, IC50: 2.4 μM

mTOR 98%
LY294002 +

p110α, IC50: 0.5 μM

+

p110β, IC50: 0.97 μM

+

p110δ, IC50: 0.57 μM

DNA-PK 99%+
AZD 6482 +

PI3Kα, IC50: 870 nM

+++

PI3Kβ, IC50: 10 nM

++

PI3Kδ, IC50: 80 nM

DNA-PK 99%+
Pictilisib ++++

p110α, IC50: 3 nM

++

p110β, IC50: 33 nM

++

p110γ, IC50: 75 nM

++++

p110δ, IC50: 3 nM

mTOR 99%+
PKI-402 ++++

PI3Kα, IC50: 2 nM

+++

PI3Kβ, IC50: 7 nM

+++

PI3Kγ, IC50: 16 nM

+++

PI3Kδ, IC50: 14 nM

mTOR 99+%
Copanlisib ++++

PI3Kα, IC50: 0.5 nM

++++

PI3Kβ, IC50: 3.7 nM

+++

PI3Kγ, IC50: 6.4 nM

++++

PI3Kδ, IC50: 0.7 nM

99%+
Omipalisib ++++

p110α, Ki: 0.019 nM

++++

p110β, Ki: 0.13 nM

++++

p110γ, Ki: 0.06 nM

++++

p110δ, Ki: 0.024 nM

99%+
Izorlisib +++

PI3Kα, IC50: 14 nM

++

PI3Kβ, IC50: 0.12 μM

++

PI3Kγ, IC50: 36 nM

+

PI3Kδ, IC50: 0.50 μM

99%+
AZD8186 ++

PI3Kα, IC50: 35 nM

++++

PI3Kβ, IC50: 4 nM

+++

PI3Kδ, IC50: 12 nM

98+%
KU-0060648 ++++

PI3Kα, IC50: 4 nM

++++

PI3Kβ, IC50: 0.5 nM

+

PI3Kγ, IC50: 0.59 μM

++++

PI3Kδ, IC50: 0.1 nM

DNA-PK 99%
Apitolisib +++

p110α, IC50: 5 nM

++

p110β, IC50: 27 nM

+++

p110γ, IC50: 14 nM

+++

p110δ, IC50: 7 nM

mTOR 98%+
CZC24832 +

PI3Kβ, IC50: 1.1 μM

++

PI3Kγ, IC50: 27 nM

98+%
BGT226 maleate ++++

PI3Kα, IC50: 4 nM

++

PI3Kβ, IC50: 63 nM

++

PI3Kγ, IC50: 38 nM

mTOR 99%+
TG 100713 ++

PI3Kα, IC50: 165 nM

+

PI3Kβ, IC50: 215 nM

++

PI3Kγ, IC50: 50 nM

+++

PI3Kδ, IC50: 24 nM

98%+
PI3K-IN-1 ++

PI3Kα, IC50: 39 nM

++

PI3Kβ, IC50: 113 nM

+++

PI3Kγ, IC50: 9 nM

++

PI3Kδ, IC50: 43 nM

mTOR,DNA-PK 98+%
TG100-115 +

PI3Kα, IC50: 1.3 μM

+

PI3Kβ, IC50: 1.2 μM

++

PI3Kγ, IC50: 83 nM

+

PI3Kδ, IC50: 235 nM

98%
PIK-90 +++

PI3Kα, IC50: 11 nM

+

PI3Kβ, IC50: 350 nM

+++

PI3Kγ, IC50: 18 nM

++

PI3Kδ, IC50: 58 nM

99%+
PIK-294 +

p110β, IC50: 490 nM

++

p110γ, IC50: 160 nM

+++

p110δ, IC50: 10 nM

99%+
Duvelisib ++++

PI3Kβ, Ki: 1564 pM

++

PI3Kγ, Ki: 243 pM

++++

PI3Kδ, Ki: 23 pM

99%+
GDC-0326 ++++

PI3Kα, Ki: 0.2 nM

++

PI3Kβ, Ki: 26.6 nM

+++

PI3Kγ, Ki: 10.2 nM

++++

PI3Kδ, Ki: 4 nM

98%
Quercetin Dihydrate +

PI3Kβ, IC50: 5.4 μM

+

PI3Kγ, IC50: 2.4 μM

+

PI3Kδ, IC50: 3.0 μM

95%
Quercetin +

PI3Kβ, IC50: 5.4 μM

+

PI3Kγ, IC50: 2.4 μM

+

PI3Kδ, IC50: 3.0 μM

Src,Sirtuin,PKC 97%
Leniolisib +

PI3Kα, IC50: 0.244 μM

+

PI3Kβ, IC50: 0.424 μM

+

PI3Kγ, IC50: 2.23 μM

+++

PI3Kδ, IC50: 0.011 μM

DNA-PK 99%+
PIK-108 98%
Eganelisib +++

PI3Kγ, IC50: 16 nM

99%+
CAY10505 98%
IPI-3063 ++++

p110δ, IC50: 2.5 nM

99%
Nemiralisib ++++

PI3Kδ, pKi: 9.9

99%+
PF-4989216 ++++

p110α, IC50: 2 nM

++

p110γ, IC50: 65 nM

++++

p110δ, IC50: 1 nM

99%+
PIK-75 HCl +++

p110α, IC50: 5.8 nM

++

p110γ, IC50: 76 nM

+

p110δ, IC50: 0.51 μM

DNA-PK 99%+
Tenalisib ++

PI3Kγ, IC50: 33.2 nM

++

PI3Kδ, IC50: 24.5 nM

95+%
Acalisib +++

p110δ, IC50: 14 nM

99%+
Umbralisib +++

PI3Kδ, IC50: 22.2 nM

99%+
AMG319 +

PI3Kγ, IC50: 850 nM

+++

PI3Kδ, IC50: 18 nM

99%
IC-87114 +

PI3Kγ, IC50: 29 μM

+

PI3Kδ, IC50: 0.5 μM

99%+
Idelalisib ++

p110γ, IC50: 89 nM

++++

p110δ, IC50: 2.5 nM

98%
PIK-293 +

p110γ, IC50: 10 μM

+

p110δ, IC50: 0.24 μM

99%+
Vps34-PIK-III +

PI3Kδ, IC50: 1.2μM

+++

Vps34, IC50: 0.018μM

99%+
GSK2292767 99+%
Seletalisib +

PI3Kγ, IC50: 282 nM

+++

PI3Kδ, IC50: 12 nM

99%+
P110δ-IN-1 ++++

P110δ, IC50: 0.6 nM

98%
PI3Kδ-IN-5 ++++

PI3Kδ, IC50: 0.9 nM

98%
SRX3207 +

PI3K alpha, IC50: 244 nM

+

PI3K gamma, IC50: 9790 nM

+

PI3K delta, IC50: 388 nM

Syk 98%
Parsaclisib HCl ++++

PI3Kδ, IC50: 1 nM

98%
IHMT-PI3Kδ-372 +++

PI3Kδ, IC50: 14 nM

98%
Trigonelline Akt 99%+
Wortmannin ++++

PI3K, IC50: 3 nM

DNA-PK,MLCK 99%+
Samotolisib DNA-PK 99%+
GNE-317 99%+
Oroxin B PTEN,Akt 99%+
NU 7026 +

PI3K, IC50: 13 μM

DNA-PK 98+%
Deguelin Akt 99%+
Ailanthone CDK,ATM/ATR,Akt 98%
Resibufogenin ROS 98%
KU-57788 +

PI3K, IC50: 5 μM

mTOR,DNA-PK 99%+
Cinobufagine Akt 98%
α-Linolenic acid 97% GC
MTX-211 EGFR 98%
PI3K/mTOR Inhibitor-2 ++++

PI3K, IC50: 3.4 nM

mTOR 99%+
SPP-86 99%+
(E)-Akt inhibitor-IV 98%
Vps34-IN-1 ++

Vps34, IC50: 25 nM

98%
SAR405 ++++

Vps34, IC50: 1.2 nM

98+%
3-Methyladenine +

PI3Kγ, IC50: 60 μM

+

Vps34, IC50: 25 μM

Autophagy 98%
Vps34-IN-4 +++

VPS34, IC50: 15 nM

98%+
Autophinib +++

Vps34, IC50: 19 nM

Autophagy 97%
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。

PIK-294 生物活性

靶点
  • p110γ

    p110γ, IC50:160 nM

  • p110β

    p110β, IC50:490 nM

  • p110δ

    p110δ, IC50:10 nM

描述 The phosphoinositide 3-kinase (PI3K)/Akt/mTOR signaling pathway is one of the most frequently dysregulated signaling cascades in human malignancies, it displays oncogenic potential and it is implicated in a wide variety of different neoplasms[3]. The PI3-K family comprises 15 kinases with distinct substrate specificities, expression patterns, and modes of regulation. The class I PI3-Ks (p110α, p110β, p110δ, and p110γ) are activated by tyrosine kinases or G protein-coupled receptors to generate PIP3, which engages downstream effectors such as the Akt/PDK1 pathway, the Tec family kinases, and the Rho family GTPases. PIK-294 is one of the most potent p110δ-selective inhibitors with IC50s of 0.01 μM for p110δ and 10 μM ,0.49 μM, 0.16 μM for p110α, p110β and p110γ[4]. In a vitro experiment, pretreatment with the PI3kinase p110δ inhibitor PIK-294 10 μM can significantly inhibited GM-CSF mediated phosphorylation in Neutrophils. The involvement of PI3Kδ in chemotaxis as pre-treatment of the cells with the PI3Kδ selective inhibitor PIK-294 significantly reduced migration in response to stimulation with CXCL8[5].

PIK-294 参考文献

[1]Bobrovnikova-Marjon E, Pytel D, et al. PERK utilizes intrinsic lipid kinase activity to generate phosphatidic acid, mediate Akt activation, and promote adipocyte differentiation. Mol Cell Biol. 2012 Jun;32(12):2268-78.

[2]Knight ZA, Gonzalez B, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

[3]Chang KY, Tsai SY, Wu CM, Yen CJ, Chuang BF, Chang JY. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin Cancer Res. 2011 Nov 15;17(22):7116-26. doi: 10.1158/1078-0432.CCR-11-0796. Epub 2011 Oct 5. PMID: 21976531.

[4]Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B, Balla T, Weiss WA, Williams RL, Shokat KM. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. doi: 10.1016/j.cell.2006.03.035. Epub 2006 Apr 27. PMID: 16647110; PMCID: PMC2946820.

[5]Martin KJ, Muessel MJ, Pullar CE, Willars GB, Wardlaw AJ. The role of phosphoinositide 3-kinases in neutrophil migration in 3D collagen gels. PLoS One. 2015 Feb 6;10(2):e0116250. doi: 10.1371/journal.pone.0116250. Erratum in: PLoS One. 2015;10(7):e0134924. PMID: 25659107; PMCID: PMC4320071.

PIK-294 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.21mL

2.04mL

1.02mL

20.43mL

4.09mL

2.04mL

PIK-294 技术信息

CAS号900185-02-6
分子式C28H23N7O2
分子量 489.528
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(214.49 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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