1. Apoptosis
  2. Bcl-2 Family
  3. BM-1197

BM-1197 (UBX1967) is a potent and selective inhibitor of dual Bcl-2/Bcl-xL, with IC50s of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo.

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BM-1197 Chemical Structure

BM-1197 Chemical Structure

CAS No. : 1391107-89-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 3361 In-stock
Solution
10 mM * 1 mL in DMSO USD 3361 In-stock
Solid
1 mg USD 670 In-stock
5 mg USD 1650 In-stock
10 mg USD 2700 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

BM-1197 (UBX1967) is a potent and selective inhibitor of dual Bcl-2/Bcl-xL, with IC50s of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo[1][2].

IC50 & Target[1]

Bcl-2

3.5 nM (IC50)

Bcl-xL

5.2 nM (IC50)

In Vitro

BM-1197 (2-2000 nM; 3 d) has marginal cytotoxicity against wild-type mouse embryonic fibroblast (MEF) cells but exerts potent growth-inhibitory activity in the MCL1−/− cells[1].
BM-1197 shows potent growth-inhibitory activities in 7 small cell lung cancer (SCLC) cell lines with IC50s <100 nM, moderate activity in 3 SCLC cell lines with IC50s of ∼600 nM and weak activity in 2 SCLC cell lines with IC50s >2000 nM[1].
BM-1197 (100 nM; 16 h) potently induces apoptosis in H146 cells[1].
BM-1197 (100 nM; 2 h) disrupts the association between Bcl-xl and Puma or Bim in H146 cells[1].
BM-1197 (100 nM; 0.5-2 h) induces Bax translocation, and it (3-30 nM; 2 h) induces cytochrome c release in H146 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MEF/MCL1−/− cells
Concentration: 2, 20, 200, 2000 nM
Incubation Time: 3 days
Result: Inhibited MCL1−/− cells proliferation.

Apoptosis Analysis[1]

Cell Line: H146 cells
Concentration: 100 nM
Incubation Time: 16 hours
Result: Induced apoptosis in a strictly Bax/Bak-dependent manner.

Western Blot Analysis[1]

Cell Line: H146 cells
Concentration: 100 nM
Incubation Time: 2 hours
Result: Attenuated the associations between Bcl-xL and BimEL or Puma.
In Vivo

BM-1197 (10 mg/kg; i.v. daily 5 days per week for 2 weeks) results in rapid and complete tumor regression in all 8 mice in H146 and H1963 tumor model[1].
BM-1197 (15 mg/kg; i.v.) causes thrombocytopenia in mice but the effect is reversible even at highly efficacious doses[1].
BM-1197 (10 mg/kg; i.v. qd) exerts a strong anti-tumor effect and is well tolerated in OCI-Ly8 xenograft models[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice bearing H146 cells[1]
Dosage: 10 mg/kg
Administration: I.v. daily 5 days per week for 2 weeks
Result: Remained tumor free for at least 32 days after the end of the treatment.
Molecular Weight

1131.78

Formula

C53H59ClF4N6O7S4

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

C[S](=O)(C(C(C1=CC(N2CCN(C(C=C3)=CC=C3N[S](=O)(C(C=C4)=CC([S](C(F)(F)F)(=O)=O)=C4N[C@@H](CSC5=CC=CC=C5)CCN(CC6)CCC6O)=O)CC2)=CC(F)=C1)=C(C(C=C7)=CC=C7Cl)N8C(C)C)=C8C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (220.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8836 mL 4.4178 mL 8.8356 mL
5 mM 0.1767 mL 0.8836 mL 1.7671 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.43%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8836 mL 4.4178 mL 8.8356 mL 22.0891 mL
5 mM 0.1767 mL 0.8836 mL 1.7671 mL 4.4178 mL
10 mM 0.0884 mL 0.4418 mL 0.8836 mL 2.2089 mL
15 mM 0.0589 mL 0.2945 mL 0.5890 mL 1.4726 mL
20 mM 0.0442 mL 0.2209 mL 0.4418 mL 1.1045 mL
25 mM 0.0353 mL 0.1767 mL 0.3534 mL 0.8836 mL
30 mM 0.0295 mL 0.1473 mL 0.2945 mL 0.7363 mL
40 mM 0.0221 mL 0.1104 mL 0.2209 mL 0.5522 mL
50 mM 0.0177 mL 0.0884 mL 0.1767 mL 0.4418 mL
60 mM 0.0147 mL 0.0736 mL 0.1473 mL 0.3682 mL
80 mM 0.0110 mL 0.0552 mL 0.1104 mL 0.2761 mL
100 mM 0.0088 mL 0.0442 mL 0.0884 mL 0.2209 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BM-1197
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