货号:A393898
同义名:
XL765;SAR245409
Voxtalisib is a potent and highly selective inhibitor of class I PI3Ks with IC50 of 39/110/9/43 nM for PI3Kα/β/γ/δ, also inhibits mTOR with IC50 of 160-910 nM.
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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 |
99%+ | |||||||||||||||||
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 |
99%+ | |||||||||||||||||
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 |
99%+ | |||||||||||||||||
Tacrolimus | ✔ | 98% | |||||||||||||||||
PP121 |
++
mTOR, IC50: 13 nM |
VEGFR,PDGFR | 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 |
99%+ | |||||||||||||||||
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 | 99%+ | ||||||||||||||||
PI3K-IN-1 |
+
mTOR, IC50: 157 nM |
99%+ | |||||||||||||||||
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 | 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,PKC,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 | ✔ | 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 |
DNA-PK,MLCK | 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 | Activation of the PI3K (phosphoinositide 3-kinase) pathway is a frequent occurrence in human tumors and is thought to promote growth, survival, and resistance to diverse therapies. Voxtalisib (XL765) is a potent and highly selective pan inhibitor of class I PI3Ks (α, β, γ, and δ) with activity against mTOR. In cellular assays, XL765 inhibits the formation of PIP3 in the membrane, and inhibits phosphorylation of AKT, p70S6K, and S6 phosphorylation in multiple tumor cell lines with different genetic alterations affecting the PI3K pathway. XL765 displayed potent inhibitory activity against class I PI3K isoforms p110α, p110β, p110δ, and p120γ, with IC50 values of 39, 110, 43, and 9 nM, respectively, IC50 values of 160 and 910 nM for mTORC1 and mTORC2, respectively. In a vitro study, XL765 inhibits colony growth with an IC50 value of 270 nM in PC-3 cells and 230 nM in MCF7 cells. Oral administration of XL765 (10, 30, 100, or 300 mg/kg) caused a dose-dependent decrease of phosphorylation of AKT, p70S6K, and S6 in the tumors on melanoma xenograft mice, reaching a maximum of 84% inhibition of S6 phosphorylation at 30 mg/kg at 4h[3]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.70mL 0.74mL 0.37mL |
18.50mL 3.70mL 1.85mL |
37.00mL 7.40mL 3.70mL |
CAS号 | 934493-76-2 |
分子式 | C13H14N6O |
分子量 | 270.29 |
别名 | XL765;SAR245409 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 9 mg/mL(33.3 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 |