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BTSA1

Cat. No. M6256
BTSA1 Structure
Size Price Availability Quantity
5mg USD 270 In stock
10mg USD 450 In stock
25mg USD 900 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: BTSA1 has no capacity to directly activate the pro-apoptotic homolog BAK. BTSA1 treatment potently and dose-responsively induces membrane translocation of recombinant soluble BAX to mitochondrial membrane, which is followed by induction of BAX oligomerization. BTSA1-induced BAX activation promotes apoptosis in cancer cells. BTSA1 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 leukemia (AML) xenografts and increases host survival without toxicity. It is well-tolerated in mice. BTSA1 has no toxic effects on healthy hematopoiesis, including healthy stem cellenriched (LSK) cells, common myeloid progenitors, granulocyte-monocyte progenitors, and megakaryocyte-erythrocyte progenitors. BTSA1 has substantial half-life in mouse plasma (T1/2 = 15 hr) and oral bioavailability (%F = 51), while a 10 mg/kg dose reaches sufficient levels (~15 μM) of BTSA1 to induce BAX activation and apoptosis in leukemia cells. Thus, BTSA1 is orally bioavailable with excellent pharmacokinetics, has significant anti-tumor activity in leukemia xenografts by promoting apoptosis, and at therapeutically effective doses it does not show any detectable toxicity in the hematopoietic system or other tissues.

Protocol
Cell Experiment
Cell lines AML cells
Preparation method AML cells (2 × 10^4 cells/well) are seeded in 96-well white plates and incubated with serial dilutions of BTSA1 or BTSA2 or vehicle (0.15% DMSO) in no FBS media for 2.5 hr, followed by 10% FBS replacement to a final volume of 100 μl. Cell viability is assayed at 24 h
Concentrations
Incubation time 2.5 h
Animal Experiment
Animal models 6-8 weeks old NOD-SCID IL2Rg null (NSG) mice/6-8 weeks old ICR (CD-1) male mice
Formulation 1% DMSO, 30% PEG-400, 65% D5W (5% dextrose in water), 4% Tween-80
Dosages 10 mg/kg
Administration oral gavage or intravenous injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 430.51
Formula C21H14N6OS2
CAS Number 314761-14-3
Purity >98%
Solubility 81 mg/mL in DMSO
Storage at -20°C
References

Direct Activation of BAX by BTSA1 Overcomes Apoptosis Resistance in Acute Myeloid Leukemia.
Reyna DE, et al. Cancer Cell. 2017 Oct 9;32(4):490-505. PMID: 29017059.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BTSA1 supplier, Bcl-2, inhibitors

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