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Home  All Products |
| All Products >>PI3K // mTOR |
| CAS NO. |
Products Name |
| 1013101-36-4 |
PF06491502 |
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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 in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. |
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| 1174428-47-7 |
SF2523 |
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| SF2523 is a highly selective and potent inhibitor of PI3Kα and BRD4 with IC50 values of 16 and 241 nM for PI3Kα and BD1, respectively |
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| 1252594-99-2 |
ETP-46321 |
more... |
| ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM for p110α/p110β; exhibits potency on mutated p110α(IC50=1.77-2.33 nM, p110a E542K; E545K; H1047R). IC50 value: 2.3/14.2 nM(p110α/p110β) Target: PI3K α/δ inhibitor ETP-46321, has been pro?led and shown to be a potent PI3K a and d inhibitor, highly selective versus mTOR and 288 representative kinases. The compound demonstrated a good pharmacokinetic profile in mice and was selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-Ras G12V oncogenic mutation, showing significant tumor growth inhibition (ca. 51%), and reduction of the tumor metabolic activity as measured by PET techniques. |
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| 1252594-99-2 |
ETP-46321 |
more... |
| ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM for p110α/p110β; exhibits potency on mutated p110α(IC50=1.77-2.33 nM, p110a E542K; E545K; H1047R). IC50 value: 2.3/14.2 nM(p110α/p110β) Target: PI3K α/δ inhibitor ETP-46321, has been pro?led and shown to be a potent PI3K a and d inhibitor, highly selective versus mTOR and 288 representative kinases. The compound demonstrated a good pharmacokinetic profile in mice and was selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-Ras G12V oncogenic mutation, showing significant tumor growth inhibition (ca. 51%), and reduction of the tumor metabolic activity as measured by PET techniques. |
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| 900185-02-6 |
PIK294 |
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| PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, less potent to PI3Kα/β/γ. IC50 value: 10 nM(p110δ) [1] Target: p110δ inhibitor PIK-294 shows distinct patterns of isoform selectivity to inhibit different subsets of class I PI3K isoforms (p110β, p110δ, and p110γ) and exhibits low sensitivity to p110α with IC50 of 10 μM). The m-phenol moiety of PIK-294 is able to penetrate the deep-affinity pocket of the ATP binding site, and thus increases in vitro inhibitory activity |
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| 1013101-36-4 |
PF-04691502 |
more... |
| PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity. PF-04691502 inhibits human and mouse PI3Kα with Ki of 1.8 and 1.2 nM, respectively, human PI3K isoforms β, δ, and γ with Ki of 2.1, 1.6, and 1.9 nM, respectively, and human mTOR with Ki of 16 nM. |
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| 1220699-06-8 |
PF-04979064 |
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| PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively. |
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| 19545-26-7 |
Wortmannin |
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| Wortmannin (SL-2052) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. wortmannin (SL-2052) also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively |
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| 1616413-96-7 |
UCB9608 |
more... |
| UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent |
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| 1354690-24-6 |
Leniolisib |
more... |
| 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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