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.
| Molecular Weight | 423.51 |
| Formula | C24H29N3O4 |
| CAS Number | 1821496-27-8 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
[1] Han B, et al. Cancer Cell. Small-Molecule Bcl2 BH4 Antagonist for Lung Cancer Therapy.
[2] Deng J, et al. Oncotarget. BCL2-BH4 antagonist BDA-366 suppresses human myeloma growth.
| Related Bcl-2 Products |
|---|
| BAD (103-127) (human)
BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL. |
| Bim BH3, Peptide IV
Bim BH3, Peptide IV is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins. |
| Bax inhibitor peptide, negative control
Bax inhibitor peptide, negative control is a inhibitor of Bax. |
| Bad BH3 (mouse)
Bad BH3 (mouse) is a biological active peptide. |
| Bid BH3 (80-99)
Bid BH3 (80-99) is a biological active peptide. |
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