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Chemical Structure| 852808-04-9 Chemical Structure| 852808-04-9

Structure of ABT-737
CAS No.: 852808-04-9

Chemical Structure| 852808-04-9

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CAS No.: 852808-04-9

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ABT-737 is a selective Bcl-2 family protein inhibitor that effectively inhibits Bcl-2, Bcl-xL, and Bcl-w with IC50 values of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 is primarily used to study apoptosis, anticancer therapy, and to enhance tumor sensitivity to chemotherapy drugs.

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Product Details of ABT-737

CAS No. :852808-04-9
Formula : C42H45ClN6O5S2
M.W : 813.43
SMILES Code : CN(CC[C@@H](NC1=CC=C(C=C1[N+]([O-])=O)S(NC(C2=CC=C(C=C2)N3CCN(CC3)CC4=CC=CC=C4C5=CC=C(C=C5)Cl)=O)(=O)=O)CSC6=CC=CC=C6)C
MDL No. :MFCD12756212
InChI Key :HPLNQCPCUACXLM-PGUFJCEWSA-N
Pubchem ID :11228183

Safety of ABT-737

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target

  • Bcl-xL

    Bcl-xL, EC50:78.7 nM

  • Bcl-B

    Bcl-B, EC50:1.82 μM

  • Bcl-w

    Bcl-w, EC50:197.8 nM

  • Bcl-2

    Bcl-2, EC50:30.3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Meg-01 cells 20 μM ABT-737 significantly sensitized Meg-01 cells to IR-induced apoptosis PMC10729570
HLE cells 5 μM 8 h ABT-737 in combination with sorafenib did not significantly increase cell death in HLE cells. PMC8313681
HUVEC cells 500 nM 2 h ABT-737 significantly reduced tubule formation in HUVEC cells PMC2756330
MCF10A cells 100 nM 24 h To test the apoptotic effect of ABT-737 in combination with AMPK activator A-769662, results showed that ABT-737 combined with A-769662 significantly enhanced apoptosis when MYC was activated. PMC6365524
T-ALL cell lines 0.8 μM 48 h To detect ABT-737-induced apoptosis, results showed that Fbw7-deficient T-ALL cells were resistant to ABT-737 PMC3076007
Huh7 cells 5 μM 8 h ABT-737 in combination with sorafenib significantly reduced cell viability and increased caspase activation in Huh7 cells. PMC8313681
Hep3B cells 5 μM 8 h ABT-737 in combination with sorafenib significantly increased cell death and caspase activation in Hep3B cells. PMC8313681
H460 cells 500 nM 2 h ABT-737 induced caspase-3 cleavage, promoting apoptosis in H460 cells and significantly enhancing their sensitivity to radiation PMC2756330

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NPG mice T-ALL mouse model Intravenous injection 40 mg/kg Twice a week for 4 weeks To evaluate the efficacy of IRAK/ABT-NP in T-ALL mouse model, results showed that IRAK/ABT-NP significantly restored white blood cell count in peripheral blood and improved the survival time of mice PMC5673049
Mice Radiation injury-induced thrombocytopenia model Intraperitoneal injection 30 mg/kg Immediately administered, duration not specified ABT-737 significantly sensitized mice to IR-induced apoptosis, leading to a significant decline in platelet counts and size PMC10729570
Mice WapMyc breast cancer model Intraperitoneal injection 100 mg/kg Once daily for 21 days To evaluate the antitumor effect of ABT-737 in the WapMyc breast cancer model, results showed that ABT-737 inhibited tumor growth in the early stages of treatment but did not significantly improve survival. PMC6365524
Mice TDI-induced asthma model Intranasal administration 4 mg/kg Administered 2 hours after each challenge ABT-737 significantly alleviated neutrophil recruitment by promoting apoptosis, thereby mitigating TDI-induced airway inflammation PMC7225000
Mice TDI-induced asthma model Intranasal administration 4 mg/kg After each challenge ABT-737 significantly alleviated neutrophil recruitment by promoting apoptosis, thereby mitigating TDI-induced airway inflammation. PMC7225000
Nude mice H460 lung cancer xenograft model Intraperitoneal injection 20 mg/kg Once daily for 7 consecutive days The combination of ABT-737 and rapamycin significantly extended tumor growth delay, increased caspase-3 activity, and reduced p62 protein levels, indicating enhanced apoptosis and autophagy PMC2756330

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01440504 - Completed - France ... More >> Centre Fran?ois Baclesse Caen, France, 14076 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.23mL

0.25mL

0.12mL

6.15mL

1.23mL

0.61mL

12.29mL

2.46mL

1.23mL

References

 

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