PI3K
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB08675 | XL765 Analogue | 1349796-36-6 | XL765 analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM, and also inhibits DNA-PK and mTOR. |
| FB01602 | XL147 | 934526-89-3 | XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC50 values of 39 nM/383 nM/36 nM/23 nM for PI3Kα/β/δ/γ, respectively and less potent to PI3Kβ. |
| FB01276 | VS-5584 | 1246560-33-7 | VS-5584 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. |
| FB01550 | Voxtalisib | 934493-76-2 | 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. |
| FB08636 | TG 100713 | 925705-73-3 | TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM. |
| FB08894 | TG 100115 | 677297-51-7 | TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. |
| FB07883 | SAR405 | 1523406-39-4 | SAR405 is highly potent and selective inhibitor of PIK3C3 with an IC50 of 27 nM. |
| FB07885 | RP-5264 | 1532533-67-7 | RP-5264 is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively. |
| FB00636 | PQR309 | 1225037-39-7 | PQR309 is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. |
| FB00685 | PKI-587 | 1197160-78-3 | PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM, 5.4 nM and 1.6 nM for PI3Kα, PI3Kγ and mTOR, respectively. |
| FB07011 | PKI-402 | 1173204-81-3 | 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. |
| FB08895 | PIK-90 | 677338-12-4 | PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ (IC50= 350 nM). |
| FB08935 | PIK-294 | 900185-02-6 | PIK-294 is a potent and selective p110δ inhibitor with IC50 of 10 nM while 10,000/490/160 nM for p110α/β/γ. |
| FB09115 | PI3Kγ Inhibitor 1 | 1172118-03-4 | PI3Kγ inhibitor 1 is a potent PI3Kγ inhibitor. |
| FB01427 | PI-3065 | 955977-50-1 | PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, > 70-fold selectivity over other PI3K family members. |
| FB01680 | PI-103 HCl | 371935-79-4 | PI-103 HCl is a potent PI3K/Akt and mTOR inhibitor with IC50 values of 2 nM for recombinant PI3K isoform p110α and 30 nM for mTOR. |
| FB02704 | PF-4989216 | 1276553-09-3 | 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. |
| FB02147 | PF-04691502 | 1013101-36-4 | 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. |
| FB08129 | NVP-BKM120 HCl | 1312445-63-8 | NVP-BKM120 Hcl(BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. |
| FB08622 | NVP-BGT226 | 1245537-68-1 | NVP-BGT226 is a class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. |
| FB08923 | NVP-BAG956 | 853910-02-8 | NVP-BAG956 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. |
| FB02695 | MLN1117 | 1268454-23-4 | MLN1117 is a selective p110α inhibitor with IC50 of 15 nM. |
| FB08480 | KU-0060648 | 881375-00-4 | KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, and with less inhibition of PI3Kγ with IC50 of 0.59 μM. |
| FB08797 | IC-87114 | 371242-69-2 | IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay. |
| FB01137 | HS-173 | 1276110-06-5 | HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM. |
| FB00943 | GSK2636771 | 1372540-25-4 | GSK2636771 is a potent, selective and orally bioavailable PI3Kβ inhibitor. It has been used in trials studying the treatment of CANCER, LYMPHOMA, Solid Neoplasm, Recurrent Solid Neoplasm, and Advanced Malignant Neoplasm, among others. |
| FB00706 | GSK1059615 | 958852-01-2 | 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 |
| FB01942 | GNE-493 | 1033735-94-2 | 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. |
| FB08064 | GNE-477 | 1032754-81-6 | GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Ki of 21 nM for mTOR. |
| FB08597 | GDC-0980 | 1032754-93-0 | GDC-0980 is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays |
| FB10690 | GDC-0032 | 1282512-48-4 | GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, > 10 fold selective over PI3Kβ. |
| FB02672 | ETP-46321 | 1252594-99-2 | ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM for p110α/p110β and exhibits potency on mutated p110α(IC50=1.77-2.33 nM, p110a E542K and E545K and H1047R). |
| FB02688 | Duvelisib R-Enantiomer | 1261590-48-0 | Duvelisib R-enantiomer is a selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM. |
| FB09243 | Duvelisib | 1201438-56-3 | Duvelisib is a 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. |
| FB05766 | Dehydroglyasperin C | 199331-35-6 | Dehydroglyasperin C, a natural product isolated and purified from the roots of Glycyrrhiza uralensis Fisch, suppresses TPA-induced cell transformation through direct inhibition of MKK4 and PI3K. |
| FB08610 | CZC-24832 | 1159824-67-5 | CZC-24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and > 100-fold selectivity over PI3Kα and PI3Kδ. |
| FB07339 | Copanlisib | 1032568-63-0 | Copanlisib is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM. |
| FB02703 | CNX-1351 | 1276105-89-5 | CNX-1351 is a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα with IC50 of 6.8 nM and 20-400 times less potent against β, γ, and δ. |
| FB08300 | CH5132799 | 1007207-67-1 | CH5132799 inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM, and is less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. |
| FB09524 | CAL-101 | 870281-82-6 | CAL-101 is a selective p110δ inhibitor with IC50 of 2.5 nM, shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. |
| FB03062 | BKM-120 | 944396-07-0 | BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. |
| FB01937 | BEZ235 Tosylate | 1028385-32-1 | BEZ235 tosylate is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. |
| FB02398 | BEBT-908 | 1235449-52-1 | BEBT-908 is a PI3Kα inhibitor with an IC50 < 0.1 μM, and also inhibits HDAC (0.1 μM ≤ IC50 ≤ 1 μM) . |
| FB01552 | AZD8835 | 1620576-64-8 | AZD8835 ia a mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM). |
| FB08325 | AZD8186 | 1627494-13-6 | AZD8186 is an isoform-specific small-molecule PI3K inhibitor, potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC50=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM). |
| FB02028 | AS-605240 | 648450-29-7 | AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively. |
| FB08936 | AS-252424 | 900515-16-4 | AS-252424 is a potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β. |
| FB08337 | AMG-319 | 1608125-21-8 | AMG-319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, > 47-fold selectivity over other PI3Ks. |
| FB09377 | Alpelisib | 1217486-61-7 | Alpelisib is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, liitle or no effect on PI3Kβ/γ/δ. |
| FB01437 | A66 | 1166227-08-2 | A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, > 100 fold selectivity for p110α over other class-I PI3K isoforms. |