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| 10mg |
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| 25mg |
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Purity: ≥98%
BDA-366 (BDA366) is a potent and specific small-molecule antagonist of the Bcl2-BH4 domain with potential anticancer activity. High affinity and selectivity are displayed in its binding to BH4. A promising anticancer target, Bcl2's BH4 domain is necessary for the protein's antiapoptotic function. Bcl2 loses its ability to prevent apoptosis when it binds to BDA-366, changing it from a survival molecule to one that triggers cell death. At effective doses, BDA-366 inhibits the growth of lung cancer xenografts made from patient cells and cell lines without significantly harming normal tissue. In lung cancer cells and tumor tissues from clinical trial participants, mTOR inhibition induces an upregulation of Bcl2. Lung cancer is effectively treated in vivo when BDA-366 and RAD001 are combined. The creation of this Bcl2-BH4 antagonist might offer a method for enhancing lung cancer treatment outcomes.
| Targets |
Bcl2-BH4 (Ki = 3.3 nM)
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| ln Vitro |
BDA-366 triggers a conformational change in BCL2, which causes strong apoptosis in primary and MM(Multiple Myeloma) cell lines. Lung cancer cell growth is inhibited both in vitro and in vivo by BDA-366, which causes a conformational change in the BCL2 molecule that changes it into a death protein[1]. As evidence of the exclusivity of its Bcl2 binding, BDA-366 did not bind to other Bcl2 family members, such as Bcl-XL, Mcl-1, or Bfl-1/A1. Calcium (Ca2+) release is induced by BDA-366 by inhibiting the interaction between Bcl2/IP3R and apoptotic cells in a Bax-dependent manner[2].
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| ln Vivo |
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| Enzyme Assay |
BDA-366 is a potent and selective small-molecule antagonist of the Bcl2-BH4 domain, it binds to BH4 with high affinity and selectivity. The antiapoptotic function of Bcl2 is dependent on the BH4 domain, making it a promising anticancer target. BCL2's prosurvival function was lost when BDA-366 caused a conformational change that exposed the BH3 domain, turning BCL2 into a prodeath protein. BDA-366 binds to BCL2 with high affinity in both non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cells. By activating BAX and releasing cytochrome c in a BCL2-dependent manner, BDA-366 induced apoptosis. BDA-366 decreased Bcl2/IP3R binding in H460 cells, which led to an increase in Ca2+ release.
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| Cell Assay |
BDA366 was applied to the human MM cell lines RPMI8226 and U266 for 48 hours at progressively higher concentrations (0, 0.1, 0.25, 0.5μM). After being collected, the cells were stained with Annexin V and PI and then analyzed using FACS. On the population of Annexin V-positive cells, apoptotic cells were gated. Early apoptotic cells were identified as Annexin V+PI+, late apoptotic cells as Annexin+PI+, and necrotic cells as AnnexinPI+.
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| References |
| Molecular Formula |
C24H29N3O4
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| Molecular Weight |
423.5
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| Exact Mass |
454.24024751
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| CAS # |
1821496-27-8
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| Related CAS # |
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| SMILES |
CCN(CC)C[C@H](CNC1=C2C(=C(C=C1)NC[C@H]3CO3)C(=O)C4=CC=CC=C4C2=O)O
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| InChi Key |
JYOOEVFJWLBLKF-HOTGVXAUSA-N
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| InChi Code |
InChI=1S/C24H29N3O4/c1-3-27(4-2)13-15(28)11-25-19-9-10-20(26-12-16-14-31-16)22-21(19)23(29)17-7-5-6-8-18(17)24(22)30/h5-10,15-16,25-26,28H,3-4,11-14H2,1-2H3/t15-,16-/m0/s1
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| Chemical Name |
1-[[(2S)-3-(diethylamino)-2-hydroxypropyl]amino]-4-[[(2S)-oxiran-2-yl]methylamino]anthracene-9,10-dione
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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