CAS NO. |
Products Name |
1032754-93-0 |
GDC-0980 (RG7422) |
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GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases. Phase 2 |
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1013101-36-4 |
PF-04691502 |
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PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. Phase 2. |
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1222998-36-8 |
Torin 1 |
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Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM; exhibits 1000-fold selectivity for mTOR than PI3K |
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1224844-38-5 |
INK 128 (MLN0128) |
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INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1 |
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1092351-67-1 |
PP242 |
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PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively |
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371935-74-9 |
PI-103 |
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PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM |
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915019-65-7 |
BEZ235 (NVP-BEZ235, Dactolisib) |
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BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively. Inhibits ATR with IC50 of 21 nM; shown to be poor inhibitory to Akt and PDK1. Phase 1/2 |
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938440-64-3 |
KU-0063794 |
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KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM; no effect on PI3Ks |
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1009298-09-2 |
AZD8055 |
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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 |
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