CHIR-124 is a novel and potent chk1 inhibitor with an IC50 of 0.3 nM. CHIR-124 interacts synergistically with camptothecin in causing growth inhibition in MDA-MB-435 cells as determined by isobologram analysis. In HCT116 human colon carcinoma cells, CHIR-124 increased the effect of SN-38, an active metabolite of irinotecan, in a sequence-dependent manner, with the highest induction of mitotic catastrophe and apoptosis seen when CHIR-124 was given sequentially after SN-38 pretreatment. More importantly, the enhancement of cell death by CHIR-124 was markedly increased in isogenic p53-null and p21-null HCT116 cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
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CCT241533 hydrochloride is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM.
CCT241533 is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM.
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AZD7762 hydrochloride is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively.
LY2603618 (IC-83) is a selective Chk1 inhibitor with potential anti-tumor activity.
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