|Targets||Checkpoint Kinase (Chk)|
|Description||This active molecular is an selective Checkpoint kinase 1 (Chk1) inhibitors and it enhances gemcitabine efficacy in tumor xenograft models. GDC-0425 was safe and yielded responses in patients with a variety of cancers. In Oct 2013, GDC 0425 was in phase I trials for Solid tumours and Lymphoma (late-stage disease) in USA and France. In May 2014, Genentech completed a phase I trial in Lymphoma and Solid tumours (late-stage disease) in USA and France.|
|Solubility||Soluble in DMSO|
|Application||Solid tumours and Lymphoma|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
CCT241533 (hydrochloride) is the hydrochloride salt form of CCT241533. As a potent Chk2 inhibitor, CCT241533 blocked CHK2 activity in human tumor cell lines in ...
Prexasertib, also known as LY2606368, is an ATP-competitive CHK1 inhibitor (Ki= 0.9 nmol/L), with minor activity against CHK2 and RSK with IC50= 8 nM and 9 nM r...
CCT245737 is an orally bioactive CHK1 inhibitor (IC50 of 1.4 nM), displaying >1,000-fold selectivity against CHK2 and CDK1. It potently inhibits cellular CHK1 a...
SCH900776, also known as MK-8776. is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activit...
CCT241533, a Chk2 inhibitor, has been found to improve the effect of genotoxic cancer therapies. IC50: 3 nM.
LY2603618 is a potent and selective small molecule inhibitor of Chk1 protein kinase activity in vitro (IC50=7 nM) and the first selective Chk1 inhibitor to ente...
SCH900776 S-isomer is the S-isomer form of SCH900776, which is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1. It can be used a...
CCT245737, a nitrogen heterocycle compound, has been found to be a CHK1 inhibitor that could probable be effective in antineoplastic studies. It is still under ...
This active molecular is an selective Checkpoint kinase 1 (Chk1) inhibitors and it enhances gemcitabine efficacy in tumor xenograft models. GDC-0425 was safe an...
AZD-7762 is a synthetic small molecule inhibitor of checkpoint kinases (Chks) with potential chemosensitizing activity. AZD7762 binds to and inhibits Chks, whic...
LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.
An inhibitor of CHK1 and CHK2
BML-277 is a selective APT-competitive inhibitor of the DNA damage response signaling enzyme CHK2 ( IC50 =15 nM).
PF-477736 is a proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity. Chk1 inhibitor PF-477736 inhibits...
The dihydrochloride salt form of LY2606368 which also known as prexasertib, is an inhibitor of checkpoint kinase 1 and has potential effect in antineoplastic. I...
CHIR-124 is a quinolone-based small molecule Chk1 inhibitor, that is structurally unrelated to other known inhibitors of Chk1. It potently and selectively inhib...