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BDA-366

(CAS No:1909226-00-1)
BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity.
CAS No:1909226-00-1
Molecular Weight(MW):423.5
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 1909226-00-1
Molecular formula(MF) C24H29N3O4
Molecular Weight(MW): 423.5
Alias
Solubility
In vitro DMSO 84 mg/mL (198.34 mM)
Ethanol 5 mg/mL (11.8 mM)
Water <1 mg/mL
In vivo
Biological Activity
Description BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity.
Targets
Bcl2-BH4 [2]
3.3 nM(Ki)
In vitro

BDA-366 induces robust apoptosis in MM(Multiple myeloma) cell lines and primary MM cells by inducing BCL2 conformational change. BDA-366 induces a conformational change in the BCL2 molecule that converts it to a death protein, and inhibits lung cancer growth in vitro and in vivo[1]. BDA-366 did not bind to other Bcl2 family members, including Bcl-XL, Mcl-1, or Bfl-1/A1, indicating the specificity of its Bcl2 binding. BDA-366 induces apoptotic cell death in a Bax-dependent manner and induces calcium (Ca2+) release via inhibition of Bcl2/IP3R interaction[2].

In vivo Delivery of BDA-366 substantially suppressed the growth of human MM xenografts in NOD-scid/IL2Rγ null mice, without significant cytotoxic effects on normal hematopoietic cells or body weight[1]. Also, BDA-366 suppresses lung cancer growth via induction of apoptosis in animal models. The BH4 antagonist BDA-366 exhibits potent efficacy against human lung cancer in vivo without platelet reduction[2].