BDA-366 is a BCL2 BH4 domain antagonist, that binds BH4 with high affinity and selectivity. BDA-366 induces robust apoptosis in MM cell lines and primary MM cells by inducing BCL2 conformational change. Delivery of BDA-366 substantially suppressed the growth of human MM xenografts in NOD-scid/IL2Rγnull mice, without significant cytotoxic effects on normal hematopoietic cells or body weight. Combined BDA-366 and RAD001 treatment exhibits strong synergy against lung cancer in vivo.
|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.
Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy.
Han B, et al. Cancer Cell. 2015 Jun 8;27(6):852-63. PMID: 26045015.
BCL2-BH4 antagonist BDA-366 suppresses human myeloma growth.
Deng J, et al. Oncotarget. 2016 May 10;7(19):27753-63. PMID: 26004684.
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