[CAS NO. 1909226-00-1] BDA-366
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PRODUCTS SPECIFICATIONS [1909226-00-1]
Store
Catalog
SLK-S7849
Brand
Selleck
CAS
1909226-00-1
DESCRIPTION [1909226-00-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 423.5 |
| Molecular Formula | C24H29N3O4 |
| SMILES | O=C1C2=C(C=CC=C2)C(C3=C(NC[C@@H]4OC4)C=CC(NC[C@H](O)CN(CC)CC)=C13)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3613 mL | 11.8064 mL | 23.6128 mL |
| 5 mM | 0.4723 mL | 2.3613 mL | 4.7226 mL |
| 10 mM | 0.2361 mL | 1.1806 mL | 2.3613 mL |
| 50 mM | 0.0472 mL | 0.2361 mL | 0.4723 mL |
Description
BDA-366 is a small-molecule domain antagonist and binds BH4 with high affinity and selectivity. It directly binds to Bcl2 with high binding affinity (Ki =3.3 ± 0.73 nM).
Targets
| Bcl2-BH4 [2] (Cell-free assay) |
| 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. 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.
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. 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.
References
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