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Omipalisib {[allProObj[0].p_purity_real_show]}

货号:A419303 同义名: GSK2126458;GSK458

GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.

Omipalisib 化学结构 CAS号:1086062-66-9
Omipalisib 化学结构
CAS号:1086062-66-9
Omipalisib 3D分子结构
CAS号:1086062-66-9
Omipalisib 化学结构 CAS号:1086062-66-9
Omipalisib 3D分子结构 CAS号:1086062-66-9
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Omipalisib 纯度/质量文件 产品仅供科研

货号:A419303 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 mTOR mTORC1 mTORC2 其他靶点 纯度
AZD-8055 ++++

mTOR (full length), IC50: 0.8 nM

mTOR (truncated), IC50: 0.13 nM

99%+
Gedatolisib ++++

mTOR, IC50: 1.6 nM

98%
GSK1059615 ++

mTOR, IC50: 12 nM

98%
Vistusertib +++

mTOR, IC50: 2.8 nM

99%+
Torin 1 +++

mTOR, IC50: 4.32 nM

+++

mTORC1, IC50: 2 nM

++

mTORC2, IC50: 10 nM

DNA-PK 99%+
Dactolisib +++

mTOR (p70S6K), IC50: 6 nM

98+%
PI-103 +

mTOR, IC50: 30 nM

99%+
WAY-600 ++

mTOR, IC50: 9 nM

99%
Voxtalisib +

mTOR, IC50: 157 nM

99%+
PF-04691502 ++

mTOR, Ki: 16 nM

98+%
Onatasertib ++

mTOR, IC50: 16 nM

DNA-PK 99%+
Chrysophanol EGFR 98%
Samotolisib DNA-PK 99%+
Torkinib +++

mTOR, IC50: 8 nM

PDGFR,DNA-PK 99%+
Everolimus 99%+
WYE-354 +++

mTOR, IC50: 5 nM

98%
Tacrolimus 98%
PP121 ++

mTOR, IC50: 13 nM

PDGFR,VEGFR 99%+
Torin 2 ++++

mTOR, IC50: 0.25 nM

DNA-PK 99%+
Rapamycin ++++

mTOR, IC50: ~0.1 nM

98%
GDC-0349 +++

mTOR, Ki: 3.8 nM

98%
XL388 ++

mTOR, IC50: 9.9 nM

+++

mTORC1, IC50: 8 nM

+

mTORC2, IC50: 166 nM

99%+
WYE-687 +++

mTOR, IC50: 7 nM

98+%
Apitolisib +

mTOR, Ki app: 17 nM

98%+
WYE-132 ++++

mTOR, IC50: 0.19 nM

99%+
Sapanisertib ++++

mTOR, Ki: 1.4 nM

99%+
BGT226 maleate 99%+
ETP-46464 ++++

mTOR, IC50: 0.6 nM

DNA-PK 98%
PI3K-IN-1 +

mTOR, IC50: 157 nM

98+%
Zotarolimus +++

FKBP-12, IC50: 2.8 nM

99+%
OSI-027 +++

mTOR, IC50: 4 nM

+

mTORC1, IC50: 22 nM

+

mTORC2, IC50: 65 nM

99%+
Ridaforolimus ++++

mTOR, IC50: 0.2 nM

99%+
Temsirolimus +

mTOR, IC50: 1.76 μM

99%
CZ415 ++

mTOR, pIC50: 8.07

99%+
SF2523 +

mTOR, IC50: 280 nM

DNA-PK 99%+
KU-0063794 ++

mTORC1, IC50: ~10 nM

++

mTORC2, IC50: ~10 nM

99%+
Omipalisib ++++

mTORC1, Ki: 0.18 nM

++++

mTORC2, Ki: 0.3 nM

99%+
Palomid 529 99%+
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。
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。

Omipalisib 生物活性

靶点
  • p110γ

    p110γ, Ki:0.06 nM

  • p110β

    p110β, Ki:0.13 nM

  • p110α

    p110α, Ki:0.019 nM

  • p110δ

    p110δ, Ki:0.024 nM

描述 PI3K/AKT/mTOR pathway directly relates to cellular quiescence, proliferation, cancer, and longevity. There are eight PI3 kinases have been identified as classes IA, 1B, II, and III based on the sequence homology and substrate preference. Among them, class IA PI3K is composed of a heterodimer consisting of a 110 kDa catalytic subunit (p110α, p110β and p110δ) and an 85 kDa regulatory subunit[1]. GSK2126458 (Omipalisib,GSK458) is a dual PI3K/mtor inhibitor, of which Ki value on p110α/β/δ/γ, mTORC1/2 is 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM measured by HTRF In vitro Profiling Assays, respectively. In cell study, GSK2126458 caused a significant reduction in the levels of pAKT-S473, pAKT-T308 and p70S6K at low nanomolar concentrations, as well as induced a G1 cell cycle arrest and inhibited cell proliferation in a large panel of cell lines, such as T47D and BT474 breast cancer lines. GSK2126458 shows both good pharmacokinetic and pharmacodynamic properties. In animal study, it showed low blood clearance and good oral bioavailability. A single 300 μg/kg dose of GSK2126458 exhibited a dose-dependent reduction in pAKT-S473 levels in BT474 tumors implanted in mice, while five times per week for 3 weeks of oral treatment of GSK2126458 exhibited dose-dependent tumor growth inhibition[2]. Up to now, GSK2126458 is being tested in a phase I study in subjects with solid tumors or lymphoma[3].
作用机制 GSK2126458 bounded in the ATP-binding site of the PI3K[2].

Omipalisib 动物研究

Dose Mice (p.o.): min = 0.3 mg/kg[2], max = 3 mg/kg[4]
Administration p.o.
Pharmacokinetics
Animal Mice[2] Rats[2] Dogs[2] Monkeys[2]
T1/2 2.1 h 6.2 h 1.3 h 3.5 h
DNAUC 1100 ng·h/ml/mg/kg 6100 ng·h/ml/mg/kg 2400 ng·h/ml/mg/kg 2300 ng·h/ml/mg/kg
Vdss 1.0 L/kg 1.1 L/kg 0.7 L/kg 0.8 L/kg
F 1 0.81 0.8 0.49
CL 10 ml/min/kg 2.3 ml/min/kg 5.8 ml/min/kg 3.6 ml/min/kg

Omipalisib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01725139 Idiopathic Pulmonary Fibrosis Phase 1 Completed - United Kingdom ... 展开 >> GSK Investigational Site London, United Kingdom, SW3 6NP 收起 <<
NCT00972686 Solid Tumours Phase 1 Completed - United States, California ... 展开 >> GSK Investigational Site San Francisco, California, United States, 94115 United States, New Jersey GSK Investigational Site New Brunswick, New Jersey, United States, 08901 United States, North Carolina GSK Investigational Site Chapel Hill, North Carolina, United States, 27599-7600 United States, Texas GSK Investigational Site Dallas, Texas, United States, 75246 GSK Investigational Site Houston, Texas, United States, 77030 United States, Utah GSK Investigational Site Salt Lake City, Utah, United States, 84112-5550 United States, Washington GSK Investigational Site Seattle, Washington, United States, 98109 Netherlands GSK Investigational Site Amsterdam, Netherlands, 1066 CX GSK Investigational Site Utrecht, Netherlands, 3584 CX 收起 <<
NCT01248858 Cancer Phase 1 Terminated(The reason for term... 展开 >>ination was lack of tolerability and efficacy of the combination treatment) 收起 << - United States, North Carolina ... 展开 >> GSK Investigational Site Chapel Hill, North Carolina, United States, 27599-7305 United States, Tennessee GSK Investigational Site Nashville, Tennessee, United States, 37203 Canada, Ontario GSK Investigational Site Toronto, Ontario, Canada, M5G 2M9 Italy GSK Investigational Site Milano, Lombardia, Italy, 20132 收起 <<

Omipalisib 参考文献

[1]Zhao HF, Wang J, et al. Recent advances in the use of PI3K inhibitors for glioblastoma multiforme: current preclinical and clinical development. Mol Cancer. 2017 Jun 7;16(1):100.

[2]Knight SD, Adams ND, et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med Chem Lett. 2010 Jan 19;1(1):39-43.

[3]Schenone S, Brullo C, et al. ATP-competitive inhibitors of mTOR: an update. Curr Med Chem. 2011;18(20):2995-3014.

[4]Ma J, Sun Y, et al. Blockage of PI3K/mTOR Pathways Inhibits Laser-Induced Choroidal Neovascularization and Improves Outcomes Relative to VEGF-A Suppression Alone. Invest Ophthalmol Vis Sci. 2016 Jun 1;57(7):3138-44.

Omipalisib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.89mL

1.98mL

0.99mL

19.78mL

3.96mL

1.98mL

Omipalisib 技术信息

CAS号1086062-66-9
分子式C25H17F2N5O3S
分子量 505.496
别名 GSK2126458;GSK458
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 50 mg/mL(98.91 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

IP 2% DMSO+water 0.1 mg/mL clear

PO 0.5% CMC-Na 52 mg/mL suspension

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