| CAS NO. |
Products Name |
| 1166227-08-2 |
A66 |
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| A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms |
|
| 1217486-61-7 |
BYL719 |
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| BYL719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, and minimal effect on PI3Kβ/γ/δ. Phase 2 |
|
| 1246560-33-7 |
VS-5584 (SB2343) |
more... |
| VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively |
|
| 1201438-56-3 |
IPI-145 (INK1197) |
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| IPI-145 (INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM, highly selective for PI3K δ/γ than other protein kinases. Phase 2 |
|
| 1009298-09-2 |
AZD8055 |
more... |
| AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1 |
|
| 870281-82-6 |
CAL-101 (Idelalisib, GS-1101) |
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| CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Phase 3 |
|
| 1173900-33-8 |
AZD6482 |
more... |
| AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ. Phase 1 |
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| |
AZD6482（s） |
more... |
| AZD6482（s） is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ |
|
| 1276105-89-5 |
CNX-1351 |
more... |
| CNX-1351 is a selective covalent Inhibitor of PI3Kα. CNX-1351 was tested against all four of the class I PI3K enzymes α, β, γ, and δ. In an end point assay, CNX-1351 potently inhibited PI3Kα and was 20−400 times less potent against β, γ, and δ. CNX-1351 inhibit PI3Kα signaling in cells and shows prolonged inhibition consistent with a covalent mechanism of Action. CNX-1351 inhibits growth of cells dependent on PI3Kα. CNX-1351 also inhibits PI3Kα signaling in vivo and bonds to p110α |
|
| 663619-89-4 |
TGX221 |
more... |
| TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM, 1000-fold more selective for p110β than p110α. |
|
| 1372540-25-4 |
GSK2636771 |
more... |
| GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a. |
|
| 957054-30-7 |
GDC0941 |
more... |
| GDC-0941 is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). |
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