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Chemical Structure| 1228108-65-3 Chemical Structure| 1228108-65-3

Structure of Sabutoclax
CAS No.: 1228108-65-3

Chemical Structure| 1228108-65-3

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Sabutoclax is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.

Synonyms: BI-97C1

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Product Details of Sabutoclax

CAS No. :1228108-65-3
Formula : C42H40N2O8
M.W : 700.78
SMILES Code : O=C(C1=C2C=C(C)C(C3=C(C)C=C4C(C(NCC(C)C5=CC=CC=C5)=O)=C(O)C(O)=CC4=C3O)=C(O)C2=CC(O)=C1O)NCC(C)C6=CC=CC=C6
Synonyms :
BI-97C1
MDL No. :MFCD26142645
InChI Key :RAYNZUHYMMLQQA-ZEQRLZLVSA-N
Pubchem ID :46236925

Safety of Sabutoclax

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Bcl-xL

    Bcl-xL, IC50:0.31 μM

  • Bfl-1

    Bfl-1, IC50:0.62 μM

  • Mcl-1

    Mcl-1, IC50:0.20 μM

  • Bcl-2

    Bcl-2, IC50:0.32 μM

    Bfl-1, IC50:0.62 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
PANC-1 750 nM 48 h Sabutoclax induces G1-S phase cell cycle arrest PMC4453003
T315I-BV173 cells 80 nM 7-10 days Inhibited cell growth and colony formation PMC7100125
SUP-B15 cells 80 nM 7-10 days Inhibited cell growth and colony formation PMC7100125
MIA PaCa-2 750 nM 48 h Sabutoclax induces G1-S phase cell cycle arrest PMC4453003
BV173 cells 80 nM 7-10 days Inhibited cell growth and colony formation PMC7100125
AsPC-1 750 nM 48 h Sabutoclax induces G1-S phase cell cycle arrest PMC4453003
BxPC-3 500 nM 24 h To evaluate the effect of Sabutoclax and Minocycline combination on pancreatic cancer cells, results showed significant inhibition of cell proliferation and induction of cell death. PMC4453003
AsPC-1 500 nM 24 h To evaluate the effect of Sabutoclax and Minocycline combination on pancreatic cancer cells, results showed significant inhibition of cell proliferation and induction of cell death. PMC4453003
PANC-1 500 nM 24 h To evaluate the effect of Sabutoclax and Minocycline combination on pancreatic cancer cells, results showed significant inhibition of cell proliferation and induction of cell death. PMC4453003
MIA PaCa-2 500 nM 24 h To evaluate the effect of Sabutoclax and Minocycline combination on pancreatic cancer cells, results showed significant inhibition of cell proliferation and induction of cell death. PMC4453003
DU-145 cells 520 nM 48 h To evaluate the pro-apoptotic effect of BI-97C1 in combination with mda-7/IL-24 on DU-145 cells, the results showed that the combination treatment significantly promoted apoptosis. PMC3102401
PC3 cells 750 nM 48 h To evaluate the cytotoxicity of BI-97C1 on PC3 cells, the results showed that BI-97C1 significantly reduced cell survival. PMC3102401
PC-3 cells 30-3000 nM 72 h To evaluate the synergistic effect of Sabutoclax with docetaxel, results showed significant synergy between Sabutoclax and docetaxel PMC3421961

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice BC LSC engraftment model Intravenous 5 mg/kg Biweekly for 4 doses Sabutoclax inhibits BC LSC survival in the marrow niche and sensitizes them to dasatinib PMC3968867
Nude mice Subcutaneous xenograft model Intraperitoneal injection 1 mg/kg 3 times per week, continuous treatment To evaluate the effect of Sabutoclax and Minocycline combination on pancreatic cancer mouse models, results showed significant inhibition of tumor growth and extended survival. PMC4453003
NOD/SCID/IL-2R γnull mice Ph+ ALL mouse model Intraperitoneal injection 5 mg/kg Every other day for a total of seven doses (14 days) Suppressed leukemia burden PMC7100125
Athymic nude mice Subcutaneous xenograft model Intraperitoneal injection 1 mg/kg 3 times per week, until the end of the experiment Sabutoclax alone reduces tumor growth, and the effect is enhanced with the addition of Minocycline PMC4453003
Nude mice M2182 human prostate tumor xenograft model Intraperitoneal injection 3 mg/kg 3 times per week for 3 weeks To evaluate the tumor growth inhibitory effect of BI-97C1 in combination with mda-7/IL-24 on the M2182 human prostate tumor xenograft model, the results showed that the combination treatment significantly inhibited tumor growth. PMC3102401
Mice Tgfbr2ColTKO mouse model Intraperitoneal injection 5 mg/kg Three times per week for two weeks To evaluate the therapeutic effect of Sabutoclax on castrate-resistant prostate cancer, results showed Sabutoclax significantly reduced tumor volume and increased apoptosis PMC3421961

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.43mL

0.29mL

0.14mL

7.13mL

1.43mL

0.71mL

14.27mL

2.85mL

1.43mL

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