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PI3K
货号 | 产品名 | CAS号 | 信息 |
---|---|---|---|
CSN16985 | 2-Amino-N-(3-(N-(3-((2-chloro-5-methoxyphenyl)amino)quinoxalin-2-yl)sulfamoyl)phenyl)-2-methylpropanamide | 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. |
CSN17775 | Vps34-IN-1 | 1383716-33-3 | Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. |
CSN16944 | 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. |
CSN19144 | Umbralisib R-enantiomer | 1532533-69-9 | TGR-1202 R-enantiomer is the R-enantiomer of TGR-1202. TGR-1202 is a potent PI3Kδ inhibitor. |
CSN17911 | Umbralisib HCl | 1532533-78-0 | TGR-1202 HCl 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. |
CSN16414 | 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. |
CSN19738 | Seletalisib | 1362850-20-1 | Seletalisib is a potent and selective PI3 kinase inhibitor, which may be useful for the treatment of immune-inflammatory diseases, such as psoriasis amd primary Sjogren's syndrome. |
CSN17243 | Bimiralisib | 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. |
CSN16214 | 1-(4-(4-(Dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea | 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. |
CSN16550 | 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. |
CSN19206 | Vps34-PIK-III | 1383716-40-2 | 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. |
CSN16011 | 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). |
CSN16051 | 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. |
CSN18811 | PIK-293 | 900185-01-5 | 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. |
CSN17696 | PI3kδ inhibitor 1 | 1332075-63-4 | PI3Kdelta inhibitor 1 is a potent and selective inhibitor of isoform of PI3Kδ and useful for treating disorders mediated by lipid kinases such as inflammation, immunol disorders, and cancer. |
CSN17655 | 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. |
CSN16085 | 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. |
CSN17801 | ON 146040 | 1404231-34-0 | ON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways and inhibits PI3K α/δ isoforms with IC50 of 14/20 nM. |
CSN18638 | NVP-QAV-572 | 957209-68-6 | NVP-QAV-572 is a potent PI3K kianse inhibitor with IC50 of 10 nM. |
CSN16039 | 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. |
CSN17646 | Serabelisib | 1268454-23-4 | MLN1117 is a selective p110α inhibitor with IC50 of 15 nM. |
CSN16586 | 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. |
CSN18808 | Eganelisib | 1693758-51-8 | IPI-549 is a selective phosphoinositide-3-kinase (PI3K)-γ inhibitor with IC50 of 16 nM as an immuno-oncology clinical candidate. |
CSN17171 | HS-173 | 1276110-06-5 | HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM. |
CSN17131 | 2-Methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid | 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. |
CSN19221 | GSK2292767 | 1254036-66-2 | GSK2292767 is a potent and selective PI3Kδ inhibitor. |
CSN16235 | 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 |
CSN17410 | 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. |
CSN17123 | 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. |
CSN17784 | GNE-317 | 1394076-92-6 | GNE-317 is a potent PI3K/mTOR inhibitor that can cross the blood–brain barrier and shows potent suppression of the PI3K pathway in the brain of mice with intact BBB. |
CSN18636 | Pictilisib dimethanesulfonate | 957054-33-0 | GDC-0941 dimethanesulfonate is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). |
CSN20187 | GDC-0326 | 1282514-88-8 | GDC-0326 is a potent and selective inhibitor of α-Isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor). GDC-0326 achieves a very high level of selectivity over other kinases. |
CSN17773 | GDC-0084 | 1382979-44-3 | GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR. |
CSN16999 | Taselisib | 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. |
CSN17623 | 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). |
CSN17639 | 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. |
CSN17654 | 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. |
CSN19141 | CAY10505 | 1218777-13-9 | CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM. |
CSN18289 | CAL-130 Racemate | 474012-90-3 | CAL-130 racemate is a phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphoblastic leukemia (T-ALL). |
CSN17841 | CAL-130 | 1431697-74-3 | CAL-130 is a phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphoblastic leukemia (T-ALL). |
CSN17842 | CAL-130 HCl | 1431697-78-7 | CAL-130 HCl is a phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphoblastic leukemia (T-ALL). |
CSN17405 | Dactolisib 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. |
CSN17605 | 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) . |
CSN16946 | AZD-8835 | 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). |
CSN19171 | 5-((2,2-Difluorobenzo[d][1,3]dioxol-5-yl)methylene)thiazolidine-2,4-dione | 648449-76-7 | AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, showing over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and being 18-fold selective for PI3Kγ than PI3Kα. |
CSN16052 | 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. |
CSN18510 | Acalisib | 870281-34-8 | Acalisib is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM. |
CSN16673 | 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. |
CSN19217 | 740 Y-P | 1236188-16-1 | 740 Y-P is cell-permeable peptide activator of PI3K. |
CSN19389 | 3-Methyl-3H-purin-6-amine | 5142-23-4 | 3-Methyladenine is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM. |