DC7953 |
GNE-493
Featured
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GNE-493 is a potent, selective, and orally available dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/12/16/16/32 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR respectively. |
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DC9515 |
PI3K inhibitor GS1059615 |
GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
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DC7141 |
Omipalisib
Featured
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GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively. |
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DC9943 |
PI3Kδ inhibitor GS2269557 |
GSK-2269557 is a potent and selective PI3Kδ inhibitor over the closely related isoforms. |
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DC9944 |
PI3Kδ inhibitor GS2292767 |
GSK2292767 is a potent and selective PI3Kδ inhibitor. |
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DC7156 |
IC-87114
Featured
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IC-87114 was the first isoform-selective PI3K inhibitor. p110δ(IC50 = 0.13 μM) vs. p110α(IC50 = 200 μM), p110β(IC50 = 16 μM) and p110γ(IC50 = 61 μM). |
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DC7873 |
INK-055 (PI3Kγ inhibitor 1) |
INK055 is a dual PI3Kg/d inhibitor. |
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DC5072 |
Duvelisib (IPI-145, INK1197)
Featured
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Duvelisib (IPI-145) is a selective inhibitor of the p110δ isoform, exhibiting IC50 values of 2.5 nM, 27.4 nM, 85 nM, and 1602 nM for p110δ, p110γ, p110β, and p110α, respectively, highlighting its specificity and potency. |
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DC9829 |
IPI-549
Featured
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IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma. |
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DC12386 |
Leniolisib (CDZ173)
Featured
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Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders. |
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DC10754 |
LX2343
Featured
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LX-2343 is a novel non-ATP competitive PI3K inhibitor, negatively regulating AKT/mTOR signaling, thus promoting autophagy, and increasing A-beta clearance. |
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DC1058 |
LY294002
Featured
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LY294002 is a PI3K inhibitor for p110α, p110δ and p110β with IC50 of 0.5 μM, 0.57 μM and 0.97 μM, respectively. |
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DC10219 |
LY3023414
Featured
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LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. |
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DC10871 |
MTX211
Featured
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MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases. |
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DC7250 |
NVP-BAG956(BAG 956) |
NVP-BAG956(BAG 956) is a potent, ATP-competitive and selective dual PI3K and PDK1 inhibitor in vitro and in vivo,with IC50 values to be 56, 444, 34, 117 and 240 nM for PI3K p110 alpha, beta, delta and gamma and PDK1 kinases, respectively. |
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DC3133 |
NVP-BGT226 (BGT226)
Featured
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NVP-BGT226 is a novel dual PI3K/mTOR inhibitor with IC50 of 1 nM. |
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DC8527 |
PF-04979064 |
PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor developed through structure-based drug design. It inhibited mTOR, PI3Kα, β, δ and γ isoforms and AKT phosphorylation with IC50 as 2.64 nM, 0.395 nM, 0.111 nM, 0.122 nM and 28. |
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DC8395 |
PF-4989216
Featured
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PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. |
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DC7232 |
PI-103
Featured
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PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. |
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DC7628 |
PI-3065
Featured
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PI-3065 is a novel potent and selective PI3K p110δ inhibitor with IC50 of 15 nM; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mTOR. |
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DC8335 |
PQR-309(Bimiralisib)
Featured
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PI3K-IN-2 is a PI3K inhibitor, inhibits pPKB and pS6 with "++++/+++(+)" in A2058 melanoma cell. |
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DC9661 |
PIK-293
Featured
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PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively. |
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DC7234 |
PIK-294
Featured
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PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively. |
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DC1096 |
PIK90
Featured
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PIK-90 is a potent and cell permeable inhibitor of p110α, p110β, p110γ and p110δ with IC50 of 11 nM, 350 nM, 18 nM and 58 nM, respectively. |
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DC9747 |
PIK-III
Featured
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PIK-III, which is a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. |
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DC7123 |
PKI402 |
PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R. |
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DC7238 |
Gedatolisib(PKI-587)
Featured
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PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 μM for PI3K-α and mTOR, respectively. |
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DC8742 |
PP121 |
PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM. |
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DC10767 |
PQR530
Featured
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PQR530 is a selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor. |
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DC10193 |
Seletalisib
Featured
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Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM. |
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