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PI3K

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.
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