BDA-366

Catalog No.S7849 Batch:S784901

Technical Data

Formula	C₂₄H₂₉N₃O₄
Molecular Weight	423.5	CAS No.	1909226-00-1
Solubility (25°C)*	In vitro	DMSO	84 mg/mL (198.34 mM)
		Ethanol	5 mg/mL (11.8 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

BDA-366 is a small-molecule Bcl2-BH4 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^[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].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines human MM RPMI8226 and U266 cell lines Concentrations 0, 0.1, 0.25, 0.5 μM Incubation Time 48 h Method Human MM cell lines RPMI8226 and U266 were treated with BDA366 at increasing concentrations (0, 0.1, 0.25, 0.5μM) for 48hr. Cells were harvested, stained with Annexin V and propidium iodide (PI), and subjected to FACS analysis. Apoptotic cells were gated on the Annexin V positive population. Annexin V+PI− cells were early apoptotic cells, Annexin+PI+ cells were late apoptotic cells, and Annexin−PI+ cells were necrotic cells.
Animal Study:^{^[1]}	Animal Models NSG mice Dosages 10 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
human MM RPMI8226 and U266 cell lines
Concentrations
0, 0.1, 0.25, 0.5 μM
Incubation Time
48 h
Method
Human MM cell lines RPMI8226 and U266 were treated with BDA366 at increasing concentrations (0, 0.1, 0.25, 0.5μM) for 48hr. Cells were harvested, stained with Annexin V and propidium iodide (PI), and subjected to FACS analysis. Apoptotic cells were gated on the Annexin V positive population. Annexin V+PI− cells were early apoptotic cells, Annexin+PI+ cells were late apoptotic cells, and Annexin−PI+ cells were necrotic cells.

Animal Study:^{^[1]}

Animal Models
NSG mice
Dosages
10 mg/kg
Administration
i.p.

References

Selleck's BDA-366 has been cited by 1 publication

CYD0281, a Bcl-2 BH4 domain antagonist, inhibits tumor angiogenesis and breast cancer tumor growth [ BMC Cancer, 2023, 23(1):479]	PubMed: 37237269

CYD0281, a Bcl-2 BH4 domain antagonist, inhibits tumor angiogenesis and breast cancer tumor growth [ BMC Cancer, 2023, 23(1):479]

PubMed: 37237269

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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