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货号 产品名 CAS号 信息
CSN23159 TCS 2312 838823-31-7 TCS2312 is a novel potent and selective CHK1 kinase inhibitor.
CSN16539 SCH900776 (S-isomer) 891494-64-7 SCH-900776 is the S-isomer form of SCH900776, which is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highly selective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinase CDK2 (IC50 = 160 nM).
CSN20306 SAR-020106 1184843-57-9 SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC (50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G (2) arrest with an IC (50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion.
CSN26617 Prexasertib Mesylate Hydrate 1234015-57-6 Prexasertib, also known as LY2606368, is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population.
CSN26616 Prexasertib dimesylate 1234015-58-7 Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity[1][2].
CSN17165 PF 477736 952021-60-2 PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes and shows ~100-fold selectivity for Chk1 than Chk2.
CSN23027 PD 407824 622864-54-4 PD 407824 is a potent and selective inhibitor of checkpoint kinases Chk1 and Wee1 with IC50s of 47 and 97 nM respectively.
CSN23009 NSC 109555 Ditosylate 66748-43-4 NSC 109555 Ditosylate is a selective, reversible, ATP-competitive Chk2 inhibitor with IC50 of 0.2 μM.
CSN20298 MU380 2109805-78-7 MU380 is a potent selective inhibitor of CHK1 kinase possessing unusual N-trifluoromethylpyrazole pharmacophore resistant to metabolic N-dealkylation
CSN17225 Prexasertib 1234015-52-1 LY2606368 is a potent and selective ATP competitive inhibitor (IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.
CSN17600 Prexasertib dihydrochloride 1234015-54-3 LY2606368 (Prexasertib) is a selective Chk1 inhibitor with IC50 value <1nM, modest to Chk2 and Rsk with IC50 values of 8nM and <10nM.
CSN17143 Rabusertib 911222-45-2 LY2603618 is a highly selective Chk1 inhibitor with potential anti-tumor activity. In a cell-free assay, it shows an IC50 of 7 nM, approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated.
CSN21202 SB-218078 135897-06-2 Inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics.
CSN22108 CHK1 inhibitor 2097938-64-0 GDC-0575 is a potent and selective CHK1 inhibitor.
CSN23328 GDC-0575 1196541-47-5 GDC-0575 is a potent and selective CHK1 inhibitor.
CSN20165 GDC-0425 1200129-48-1 GDC-0425 is an oral, selective Chk1 inhibitor. GDC-0425 enhances gemcitabine (gem) efficacy in tumor xenograft models, and shows greater chemopotentiation in cancer cell lines lacking p53 activity.
CSN16590 CHIR-124 405168-58-3 CHIR-124 is a potent Chk1 inhibitor with IC50 of 0.3 nM with 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.
CSN18829 CCT245737 1489389-18-5 CCT245737 is a potent, ATP-competitive CHK1 inhibitor with an IC50 of 30-220 nM.
CSN18925 CCT244747 1404095-34-6 CCT244747 is potent, highly selective, orally active, ATP competitive CHK1 inhibitor with IC50 of 29-170nM.
CSN17641 CCT241533 1262849-73-9 CCT241533 is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM and shows minimal cross-reactivity against a panel of kinases at 1 μM.
CSN17848 CCT241533 hydrochloride 1431697-96-9 CCT241533 HCl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM and shows minimal cross-reactivity against a panel of kinases at 1 μM.
CSN16323 BML-277 516480-79-8 BML-277 is a selective Chk2 (checkpoint kinase 2) inhibitor with IC50 of 15 nM.
CSN15785 AZD-7762 860352-01-8 AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM, being equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.
CSN22704 (S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide hydrochloride 1246094-78-9 AZD 7762 HCl is a potent and selective ATP-competitive inhibitor of Chk1 and Chk2, both with IC50 of 5 nM.
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