BML-277 protects T cells from apoptosis by controlling the response of p53 to radiation-induced DNA breaks. This is suggestive of BML-277's use as an adjuvant for radiation therapy in cancer. BML-277 is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. It has also been found to weakly inhibit 31 other kinases.
|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.
|Solubility||DMSO 55 mg/mL|
Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.
Arienti KL,et.al. J Med Chem. 2005 Mar 24;1873-85. PMID: 15771432.
|Related Checkpoint Products|
Prexasertib dihydrochloride (LY2606368 HCl) is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase with IC50s of <1 nM and 8 nM for CHK1 and CHK2, respectively.
Ipilimumab is an immunomodulatory monoclonal antibody directed against the cell surface antigen CTLA-4 and also a type of immune checkpoint inhibitor. MW : 148 kD.
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.
AZD7762 hydrochloride is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively.
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