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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 | 99%+ | |||||||||||||||
HS-173 |
++++
PI3Kα , IC50: 0.8 nM |
99%+ | |||||||||||||||||
Serabelisib |
+++
PI3Kα, IC50: 21 nM |
99%+ | |||||||||||||||||
GNE-477 |
++++
PI3Kα, IC50: 4 nM |
mTOR | 99%+ | ||||||||||||||||
YM-201636 |
+
p110α, IC50: 3.3 μM |
PIKfyve | 99%+ | ||||||||||||||||
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 |
99%+ | ||||||||||||||||
SF2523 |
++
PI3Kα, IC50: 34 nM |
++
PI3Kγ, IC50: 158 nM |
DNA-PK,mTOR | 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 | ✔ | 99%+ | |||||||||||||||||
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 |
99%+ | ||||||||||||||
PI-103 |
++++
p110α, IC50: 2 nM |
++++
p110β, IC50: 3 nM |
+++
p110γ, IC50: 15 nM |
++++
p110δ, IC50: 3 nM |
DNA-PK,mTOR | 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 |
DNA-PK,mTOR | 99%+ | |||||||||||||
AZD-8835 |
+++
PI3Kα, IC50: 6.2 nM |
+
PI3Kβ, IC50: 431 nM |
++
PI3Kγ, IC50: 90 nM |
+++
PI3Kδ, IC50: 5.7 nM |
99%+ | ||||||||||||||
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 |
99%+ | |||||||||||||
AS-605240 |
++
PI3Kα, IC50: 60 nM |
+
PI3Kβ, IC50: 270 nM |
+++
PI3Kγ, IC50: 8 nM |
+
PI3Kδ, IC50: 300 nM |
99%+ | ||||||||||||||
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 | 99%+ | |||||||||||||
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 |
99%+ | |||||||||||||||
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 | 99%+ | |||||||||||||
CZC24832 |
+
PI3Kβ, IC50: 1.1 μM |
++
PI3Kγ, IC50: 27 nM |
99%+ | ||||||||||||||||
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 |
99%+ | ||||||||||||||
PI3K-IN-1 |
++
PI3Kα, IC50: 39 nM |
++
PI3Kβ, IC50: 113 nM |
+++
PI3Kγ, IC50: 9 nM |
++
PI3Kδ, IC50: 43 nM |
DNA-PK,mTOR | 99%+ | |||||||||||||
TG100-115 |
+
PI3Kα, IC50: 1.3 μM |
+
PI3Kβ, IC50: 1.2 μM |
++
PI3Kγ, IC50: 83 nM |
+
PI3Kδ, IC50: 235 nM |
99%+ | ||||||||||||||
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 |
98%+ | |||||||||||||||
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 | ✔ | 99%+ | |||||||||||||||||
Eganelisib |
+++
PI3Kγ, IC50: 16 nM |
99%+ | |||||||||||||||||
CAY10505 | ✔ | 99%+ | |||||||||||||||||
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 |
98%+ | ||||||||||||||||
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 |
99%+ | |||||||||||||||||
PI3Kδ-IN-5 |
++++
PI3Kδ, IC50: 0.9 nM |
99%+ | |||||||||||||||||
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 |
MLCK,DNA-PK | 99%+ | ||||||||||||||||
Samotolisib | ✔ | DNA-PK | 99%+ | ||||||||||||||||
GNE-317 | ✔ | 99%+ | |||||||||||||||||
Oroxin B | ✔ | Akt,PTEN | 99%+ | ||||||||||||||||
NU 7026 |
+
PI3K, IC50: 13 μM |
DNA-PK | 99%+ | ||||||||||||||||
Deguelin | ✔ | Akt | 99%+ | ||||||||||||||||
Ailanthone | ✔ | CDK,Akt,ATM/ATR | 98% | ||||||||||||||||
Resibufogenin | ✔ | ROS | 98% | ||||||||||||||||
KU-57788 |
+
PI3K, IC50: 5 μM |
DNA-PK,mTOR | 99%+ | ||||||||||||||||
Cinobufagine | ✔ | Akt | 98% | ||||||||||||||||
α-Linolenic acid | ✔ | 97% GC | |||||||||||||||||
MTX-211 | ✔ | EGFR | 99%+ | ||||||||||||||||
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 |
99%+ | |||||||||||||||||
3-Methyladenine |
+
PI3Kγ, IC50: 60 μM |
+
Vps34, IC50: 25 μM |
Autophagy | 98% | |||||||||||||||
Vps34-IN-4 |
+++
VPS34, IC50: 15 nM |
99%+ | |||||||||||||||||
Autophinib |
+++
Vps34, IC50: 19 nM |
Autophagy | 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。 |
靶点 |
|
描述 | The phosphatidylinositol 3-kinase (PI3K) pathway is a major focus for drug development in various cancer due to its function as a key regulator of cell growth and survival. The bromodomain and extraterminal domain (BET) family of epigenetic “reader” proteins, including BRDT, BRD2, BRD3, and BRD4, play important roles in histone acetylation-dependent transcriptional regulation. SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively[1]. In vitro, SF2523 decreased LPS- or IL4-induced MΘ polarization. At 500 nM, SF2523 significantly decreased mRNA expression of IL6 and iNos in LPS induced Bone marrow–derived macrophages (BMDMs) and gene expression of Arg, Tgfb, Vegf, Mmr, Ym1, and Fizz1 in IL4-induced BMDMs[2]. In vivo, s.c. xenograft model of MYCN-amplified neuroblastoma in immunocompromised mice treated with SF2523 (50 mg/kg, three times a week) showed a significant reduction of tumor volume compared with vehicle-treated group, without gross toxicity[1]. |
作用机制 | The structure of the BRD4 BD1–SF2523 complex reveals a characteristic four-helix bundle fold of BD1, with SF2523 occupying a deep hydrophobic pocket at one of the open ends of the bundle. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.69mL 0.54mL 0.27mL |
13.46mL 2.69mL 1.35mL |
26.92mL 5.38mL 2.69mL |
CAS号 | 1174428-47-7 |
分子式 | C19H17NO5S |
分子量 | 371.407 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 30 mg/mL(80.77 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 |