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BTSA1 Bcl-2 activator

Name: BTSA1
Brand: Selleck Chemicals
SKU: S8650
Rating: 5 (4 reviews)

Cat.No.S8650

BTSA1 is a pharmacologically optimised BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukaemia cell lines and patient samples while sparing healthy cells.

Chemical Structure

Molecular Weight: 430.51

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Quality Control

Batch: S865001 DMSO]81 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.51%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.51

Related Targets	Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Other Bcl-2 Inhibitors	Navitoclax (ABT-263) S63845 ABT-737 Obatoclax Mesylate (GX15-070) A-1331852 A-1210477 TW-37 A-1155463 Dihydrochloride AZD5991 UMI-77

Chemical Information, Storage & Stability

Molecular Weight	430.51	Formula	C₂₁H₁₄N₆OS₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	314761-14-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C(C=C1)C2=CSC(=N2)N3C(=O)C(=C(N3)C4=CC=CC=C4)N=NC5=NC=CS5

Solubility

In vitro
Batch:

DMSO : 81 mg/mL (188.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (4.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.200mg/ml (0.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Bax
In vitro	BTSA1 has no capacity to directly activate the pro-apoptotic homolog BAK. This compound treatment potently and dose-responsively induces membrane translocation of recombinant soluble BAX to mitochondrial membrane, which is followed by induction of BAX oligomerisation. This chemical-induced BAX activation promotes apoptosis in cancer cells. It reduces viability of all AML cell lines in a dose-dependent manner with IC50 values ranged between 1 and 4 μM, which leads to complete effect within 24 hr treatment. It induces dose-dependent caspase-3/7 activation in all five AML cell lines.
In vivo	BTSA1 potently suppresses human acute myeloid leukaemia (AML) xenografts and increases host survival without toxicity. It is well-tolerated in mice with no toxic effects on healthy haematopoiesis, including healthy stem cell-enriched (LSK) cells, common myeloid progenitors, granulocyte-monocyte progenitors, and megakaryocyte-erythrocyte progenitors. This compound has substantial half-life in mouse plasma (T_1/2 = 15 hr) and oral bioavailability (%F = 51), while a 10 mg/kg dose reaches sufficient levels (~15 μM) of the compound to induce BAX activation and apoptosis in leukaemia cells. Thus, it is orally bioavailable with excellent pharmacokinetics, has significant anti-tumour activity in leukaemia xenografts by promoting apoptosis, and at therapeutically effective doses it does not show any detectable toxicity in the haematopoietic system or other tissues.
References	[1] https://pubmed.ncbi.nlm.nih.gov/29017059/

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