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PI3K
货号 | 产品名 | CAS号 | 信息 |
---|---|---|---|
CSN12308 | 4,4'-(6-(2-(Difluoromethyl)-1H-benzo[d]imidazol-1-yl)-1,3,5-triazine-2,4-diyl)dimorpholine | 475110-96-4 | ZSTK474 inhibits class I PI3K isoforms with IC50s of of 16/44/4.6 and 49 nM for PΙ3Κα/β/δ and γ respectively. |
CSN15908 | PI3K-IN-1 | 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. |
CSN12670 | Pilaralisib analogue | 956958-53-5 | XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. |
CSN13854 | 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. |
CSN12315 | TGX-221 | 663619-89-4 | TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, and is 1000-fold selective for p110β than p110α. |
CSN16010 | TG100-115 | 677297-51-7 | TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. |
CSN15739 | SAR405 | 1523406-39-4 | SAR405 is highly potent and selective inhibitor of PIK3C3 with an IC50 of 27 nM. |
CSN15741 | Umbralisib | 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. |
CSN13561 | PI3Kγ inhibitor 1 | 1172118-03-4 | PI3Kγ inhibitor 1 is a potent PI3Kγ inhibitor. |
CSN13877 | 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. |
CSN13906 | 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. |
CSN17314 | PF-04979064 | 1220699-06-8 | PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with an IC50 of 9.1 nM. |
CSN13693 | Buparlisib 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. |
CSN15893 | BGT226 maleate | 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. |
CSN11484 | 3,5,7-Trihydroxy-2-(3,4,5-trihydroxyphenyl)-4H-chromen-4-one | 529-44-2 | Myricetin, a natural flavonoid isolated and purified from the root bark of Myrica cerifera L. with antioxidant and anti tumor properties, is an inhibitor of MEK1 activity and transformation of JB6 P+ mouse epidermal cells. It also inhibits PI3Kγ with Kd of 0.17 μM. |
CSN15967 | IC-87114 | 371242-69-2 | IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay. |
CSN12474 | Omipalisib | 1086062-66-9 | 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. |
CSN15869 | Apitolisib | 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 |
CSN12429 | Pictilisib | 957054-30-7 | 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). |
CSN13707 | 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. |
CSN15117 | 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. |
CSN15881 | CZC24832 | 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. |
CSN15713 | 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. |
CSN15797 | Izorlisib | 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. |
CSN12930 | (S)-2-(1-((9H-Purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one | 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. |
CSN13168 | 5-(2,6-Dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine | 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. |
CSN12260 | 2-Methyl-2-(4-(3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl)phenyl)propanenitrile | 915019-65-7 | 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 in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. |
CSN15821 | (R)-8-(1-((3,5-Difluorophenyl)amino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide | 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). |
CSN12381 | AZD 6482 | 1173900-33-8 | AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ. |
CSN13098 | 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. |
CSN15834 | AMG319 | 1608125-21-8 | AMG-319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, > 47-fold selectivity over other PI3Ks. |
CSN13709 | 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. |