货号:A281340
同义名:
GDC-0980; GNE 390
GDC-0980 is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays
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产品名称 | mTOR ↓ ↑ | mTORC1 ↓ ↑ | mTORC2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
AZD-8055 |
++++
mTOR (truncated), IC50: 0.13 nM mTOR (full length), IC50: 0.8 nM |
99%+ | |||||||||||||||||
Gedatolisib |
++++
mTOR, IC50: 1.6 nM |
99% | |||||||||||||||||
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 |
DNA-PK,PDGFR | 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 |
95% | |||||||||||||||||
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 | 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 | 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 |
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 | 98% | |||||||||||||
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 |
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 |
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 | 98% | |||||||||||||
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 | 98% | |||||||||||||
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 |
PKC,Src,Sirtuin | 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 | ✔ | 98% | |||||||||||||||||
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 |
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 | ✔ | Akt,CDK,ATM/ATR | 98% | ||||||||||||||||
Resibufogenin | ✔ | ROS | 98% | ||||||||||||||||
KU-57788 |
+
PI3K, IC50: 5 μM |
DNA-PK,mTOR | 99%+ | ||||||||||||||||
Cinobufagine | ✔ | Akt | 99% | ||||||||||||||||
α-Linolenic acid | ✔ | 99% | |||||||||||||||||
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 | 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 |
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描述 | PI3K and mTOR are two critical signaling pathways that of high degree similarity of active sites and thus are important for cell growth and cancer treatment. GDC-0980 is a class 1 PI3K and mTOR kinase inhibitor with IC50 values of 5, 27, 7 and 14 nM for PI3Kα, β, δ and γ isoforms respectively. The Ki of GDC-0980 against mTOR is 17nM. Treatment with 1 μM GDC-0980 could also show >60% inhibition to some additional kinases like Fgr, Mlk1, Syk with IC50 VALUES of 697, 232, 134 nM respectively. In PC-3 and MCF-7 neo/HER2 cell lines, treatment with 1 mg/kg of this drug demonstrated significant antitumor activity and tumor growth delay. Tumor stasis or regressions were also observed with the concentration of 7.5 mg/kg, which further showed a high cellular potency and low plasma clearance[1]. Treatment of GDC-0980 with IC50 <500nM demonstrated 100%, 78%, 88%, 67% and 33% inhibitions to prostate, breast, NSCLC, pancreatic and melanoma cell lines respectively, suggesting different reduction of viability in alternated cancer cells. Furthermore, phosphorylation of all downstream markers was reduced including phospho-Akt (at Thr308, Ser473 sites), phospho-S6 and phospho-ERK. The assessment results of cell cycle markers treated with 0.1 and 0.5 μM GDC-0980 found that Cyclin D1 expressed in most proliferating cells except for KP4 and A375 cell lines. Besides, cleaved PARP was also found in KPL4 and LoVo cell lines, suggesting an earlier apoptotic response to this drug. In a 20 xenograft tumor models, treatment of 5 mg/kg GDC-0980 resulted in 70% loss of body weight and 50% tumor growth inhibitions in 15 of the models. In pharmacokinetic mice model, 2.5 mg/kg of GDC-0980 could delay tumor growth. Tumor stasis and tumor regression were happened at higher concentrations that were 5 mg/kg and 10 mg/kg respectively. In the 2.5 mg/kg concentration group, undetectable GDC-0980 plasma levels was found as well as reduced baseline level of pAkt/tAkt that were 60% and 75% at 5 and 10 mg/kg concentration groups, suggesting GDC-0980 is an effective dual PI3K/mTOR inhibitor[2]. |
作用机制 | GDC-0980 binds to mTORC1 and mTORC2, decreasing phospho-AktThr308 and Ser473, S6K and phospho-S6[2]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
human MCF7.1 cells | Proliferation assay | Antiproliferative activity against human MCF7.1 cells expressing HER2 gene after overnight incubation by CellTiter-Glo luminescence assay, IC50=0.255 μM | 21981714 | ||
human PC3 cells | Function assay | Inhibition of PIK3 gamma-mediated Akt phosphorylation at Ser473 in human PC3 cells by ELISA, IC50=0.036 μM | 21981714 | ||
human PC3 cells | Proliferation assay | Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay, IC50=0.307 μM | 21981714 | ||
insect cells | Function assay | 30 mins | Inhibition of human recombinant mTOR expressed in insect cells assessed as phosphorylation of recombinant (GFP)-4-EBP1 measured after 30 mins by fluorescence polarization assay, Ki=0.017 μM | 21981714 | |
Dose | Mice: 0.25 mg/kg - 10 mg/kg[2] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.01mL 0.40mL 0.20mL |
10.03mL 2.01mL 1.00mL |
20.06mL 4.01mL 2.01mL |
CAS号 | 1032754-93-0 |
分子式 | C23H30N8O3S |
分子量 | 498.6 |
SMILES Code | C[C@H](O)C(N1CCN(CC2=C(C)C3=NC(C4=CN=C(N)N=C4)=NC(N5CCOCC5)=C3S2)CC1)=O |
MDL No. | MFCD20274520 |
别名 | GDC-0980; GNE 390; RG 7422 |
运输 | 蓝冰 |
InChI Key | YOVVNQKCSKSHKT-HNNXBMFYSA-N |
Pubchem ID | 25254071 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C |
溶解方案 |
DMSO: 15 mg/mL(30.08 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |
0.5% methylcellulose+0.2% Tween 80+water 30 mg/mL suspension |