货号:A117244 同义名: SL-2052;KY 12420
Wortmannin(SL-2052;KY-12420)是一种有效、选择性和不可逆的PI3K抑制剂,IC50为3 nM。它还阻止自噬形成,强效抑制Polo样激酶1(PlK1)和Plk3的IC50分别为5.8 nM和48 nM。
规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
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 |
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 | ✔ | 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 |
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 |
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 |
DNA-PK,mTOR | 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 |
Sirtuin,Src,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 | ✔ | ATM/ATR,CDK,Akt | 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 | 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。 |
产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
97% | |||||||||||||||||
Lys05 | ✔ | 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 | ATM ↓ ↑ | ATR ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Wortmannin |
++
ATM, IC50: 150 nM |
PI3K,DNA-PK,MLCK | 99%+ | ||||||||||||||||
CP-466722 |
+
ATM, IC50: 410 nM |
99%+ | |||||||||||||||||
Torin 2 |
++
ATM, EC50: 28 nM |
++
ATR, EC50: 35 nM |
DNA-PK,mTOR | 99%+ | |||||||||||||||
KU-55933 |
+++
ATM, IC50: 12.9 nM |
96% | |||||||||||||||||
ETP-46464 |
+
ATM, IC50: 545 nM |
+++
ATR, IC50: 14 nM |
DNA-PK,mTOR | 98% | |||||||||||||||
CGK733 |
++
ATM, IC50: 200 nM |
++
ATR, IC50: 200 nM |
99%+ | ||||||||||||||||
AZD0156 | ✔ | 99%+ | |||||||||||||||||
Dactolisib |
+++
ATR, IC50: 21 nM |
98+% | |||||||||||||||||
Ceralasertib |
++++
ATR, IC50: 1 nM |
99%+ | |||||||||||||||||
Berzosertib |
+++
ATR, IC50: 19 nM |
99%+ | |||||||||||||||||
VE-821 |
+++
ATR, Ki: 13 nM |
99%+ | |||||||||||||||||
AZ20 |
++++
ATR, IC50: 5 nM |
mTOR | 99%+ | ||||||||||||||||
Schizandrin B |
+
ATR, IC50: 7.25 μM |
P-gp | 98% | ||||||||||||||||
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 | DNA-PK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PI-103 |
++
DNA-PK, IC50: 23 nM |
99%+ | |||||||||||||||||
CC-115 |
+++
DNA-PK, IC50: 0.013 μM |
mTOR | 98+% | ||||||||||||||||
Samotolisib | ✔ | 99%+ | |||||||||||||||||
NU 7026 |
+
DNA-PK, IC50: 0.23 μM |
PI3K | 98+% | ||||||||||||||||
PIK-75 HCl |
++++
DNA-PK, IC50: 2 nM |
99%+ | |||||||||||||||||
PP121 |
+
DNA-PK, IC50: 60 nM |
PDGFR,VEGFR | 99%+ | ||||||||||||||||
KU-0060648 |
++++
DNA-PK, IC50: 5 nM |
99% | |||||||||||||||||
KU-57788 |
+++
DNA-PK, IC50: 14 nM |
99%+ | |||||||||||||||||
LTURM34 |
++
DNA-PK, IC50: 0.034 μM |
98%+ | |||||||||||||||||
SF2523 |
+++
DNA-PK, IC50: 9 nM |
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 | Phosphoinositide-3-kinase family (PI3Ks) phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role in recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. KY-12420, also termed wortmannin, is a PI3K inhibitor. The IC50 value of KY-12420 against PI3K was 3 nM according to purified calf PI3K assay or cell based immunoprecipitate assay. In intact cells, KY-12420 inhibited PI3K activity with an IC50 of 2 nM[3]. Post 24 h incubation, KY-12420 could sensitize melanoma cell lines A375, Mel-HO, as well as respective TRAIL resistant cell lines, for TRAIL-induced apoptosis at the concentrations of 4 μM or 8 μM, as revealed by a sub-G1 cell analysis, while KY-12420 alone was not effective[4]. In lung cancer cell lines A549 and H1703, KY-12420 at the concentration of 2.5 μM also enhanced cytotoxicity induced by tamoxifen[5]. In an orthotopic pancreatic tumor model established by injection of PK1 cells into the pancreas of SCID mice, KY-12420 plus gemcitabine was administrated via i.p. injection. The dose of KY-12420 was 0.35 mg/kg and the dose of gemcitabine was 80 mg/kg. Both of the agents were injected biweekly for a total treatment period of 5 weeks. The result turned out that KY-12420 plus gemcitabine reduced tumor weights by 5-fold relative to the vehicle control. For comparison, the group of gemcitabine alone at the same dose and schedule reduced tumor weights by 1.4-fold, and the group of KY-12420 alone failed to inhibit tumor growth[6]. |
作用机制 | Based on the X-ray crystallographic structure of KY-12420 bound to PI3Kγ in the kinase’s ATP binding pocket, KY-12420 most closely fits and fills the active site and induces a conformational change in the catalytic domain of the kinase[7]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
5637 | 10 μM | Apoptosis Assay | 40 min | reverses p21WAF1 expression, CDK expression, and cell inhibition induced by fucoidan | 24333868 |
A-375 | 4/8 μM | Apoptosis Assay | 24 h | enhances TRAIL-induced apoptosis | 24113173 |
A-375-TS | 4/8 μM | Apoptosis Assay | 24 h | enhances TRAIL-induced apoptosis | 24113173 |
A459 | 2.5 μM | Growth Inhibition Assay | 1-4 d | enhances cell growth inhibition treatment with tamoxifen | 25490383 |
Dose | Rat: 1 mg/kg[3] (i.p.) Mice: 0.2 mg/kg - 4 mg/kg[4] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.33mL 0.47mL 0.23mL |
11.67mL 2.33mL 1.17mL |
23.34mL 4.67mL 2.33mL |
CAS号 | 19545-26-7 |
分子式 | C23H24O8 |
分子量 | 428.432 |
别名 | SL-2052;KY 12420;NSC 627609;BRN 0067676 |
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: 50 mg/mL(116.7 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 |
5% DMSO+40% PEG 300+5% Tween 80+water 5 mg/mL |