Catalog |
name |
Description |
price |
R-C-990 |
Tivozanib (AV-951) cas:475108-18-0 |
Tivozanib(AV-951,KRN-951)is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM,and also inhibits PDGFR and c-Kit,low activity observed against FGFR-1,Flt3,c-Met,EGFR and IGF-1R. |
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R-C-996 |
GSK2636771 cas:1372540-25-4 |
GSK2636771 is a potent,orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ.Sensitive to PTEN null cell lines. |
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R-C-998 |
AS-252424 cas:900515-16-4 |
AS-252424 is a potent inhibitor of PI3K with selectivity for the γ isoform.It inhibits human recombinant PI3Kγ,α,β,and δ with IC50 values of 30,940, 20,000,and 20,000 nM respectively. |
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R-C-1000 |
CNX1351 cas:1276105-89-5 |
CNX-1351 is a covalent inhibitor of PI3Kα(IC50=6.8 nM).1 It is selective for PI3Kα over PI3Kβ,-γ,and-δ(IC50s=166,240.3,and 3,020 nM,respectively),as well as PI3KC2A,PI3KC,PI4Kα,PI4Kβ,SPHK1,and SPHK2 (IC50s=>1 µM for all).CNX-1351 (500 nM)inhibits phosphorylation of Akt in SKOV3 cells.It inhibits the growth of SKOV3 and MCF-7 cancer cells(GI50s=77.6 and 54.7 nM,respectively).CNX-1351(100 mg/kg)inhibits Akt phosphorylation in mouse spleen. |
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R-C-1079 |
Berzosertib (VE-822) CAS:1232416-25-9 |
VE-822 is an inhibitor of ataxia-telangiectasia mutated(ATM)Rad3-related protein kinase(ATR),a regulator of DNA damage repair, with Ki and IC50 values of <0.2 and 19 nM,respectively,in pancreatic cancer cells in vitro.1 It is selective for ATR over ATM (Ki=34 nM;IC50=2,600 nM) as well as DNA-PK,mTOR,and PI3Kγ(Kis= >4,000,>1,000,and 220 nM,respectively).In cultured COLO 205 colorectal cancer cells,VE-822(80 nM)reduces the IC50 of the topoisomerase 1 inhibitor SN-38 by at least 8-fold.2 In a mouse xenograft model,it delays the growth of radiation-treated PSN-1 pancreatic cancer xenografts by 2-3-fold relative to radiation alone when administered at a dose of 60 mg/kg.VE-822 also enhances the tumoricidal effects of cisplatin against primary human lung cancer xenografts and the effects of the topoisomerase inhibitor irinotecan against COLO 205 colorectal tumors in mice. |
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R-C-1081 |
PI3065 CAS:955977-50-1 |
PI 3065 is a p110δ-selective PI3K inhibitor with Ki and IC50 values of 1.5 nM and 5 nM,respectively.Administration of PI 3065 suppressed 4T1 tumour growth and metastasis,to a similar extent as genetic inactivation of p110δ,marked by initial tumour progression,followed by tumour regression. |
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R-C-1083 |
TORIN1 CAS:1222998-36-8 |
Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM.Torin 1 shows over 100-fold selectivity for mTOR over PI3Kα and other PI3K-like kinases, including ATM,DNA-PK,and hVps34,as well as 450 other protein kinases.Torin 1 induces autophagy in HeLa cells.Torin 1 is efficacious at a dose of 20 mg/kg in inhibiting downstream effectors of mTOR in mice.In a recent study,it is reported Torin 1 increases neurotensin secretion and gene expression through activation of the MEK/ERK/c-Jun pathway in the human endocrine cell line BON. |
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R-C-1085 |
LY2584702 CAS:1082949-67-4 |
LY2584702 inhibits ribosomal protein S6 Kinase(p70S6K),and prevents phosphorylation of the S6 subunit of ribosomes,thereby inhibiting normal ribosomal function within tumor cells leading to a decrease in protein synthesis and in cellular proliferation.LY2584702 exhibited anti-tumour activity in preclinical analysis. |
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R-C-1086 |
CHIR99021 CAS:252917-06-9 |
CHIR-99021(CT99021)is a potent and selective GSK-3α/βinhibitor with IC50s of 10 nM and 6.7 nM.CHIR-99021 shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases.CHIR-99021 is also a potent Wnt/β-catenin signaling pathway activator.CHIR-99021 enhances mouse and human embryonic stem cells self-renewal.CHIR-99021 induces autophagy. |
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R-C-1117 |
HTH-01-015 CAS:1613724-42-7 |
HTH-01-015 is a selective NUAK1/ARK5 inhibitor(IC50 is 100 nM).HTH-01-015 inhibits NUAK1 with>100-fold higher potency than NUAK2(IC50 of >10μM). |
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