[CAS NO. 1228108-65-3] Sabutoclax
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PRODUCTS SPECIFICATIONS [1228108-65-3]
Catelog
SLK-S8061
Brand
Selleck
CAS
1228108-65-3
DESCRIPTION [1228108-65-3]
Overview
| MDL | MFCD26142645 |
|---|---|
| Molecular Weight | 700.78 |
| Molecular Formula | C42H40N2O8 |
| SMILES | O=C(C1=C(O)C(O)=CC2=C(O)C(C3=C(C)C=C4C(C(NCC(C5=CC=CC=C5)C)=O)=C(O)C(O)=CC4=C3O)=C(C)C=C12)NC[C@@H](C6=CC=CC=C6)C |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
Sabutoclax (BI-97C1) is a pan-Bcl-2 inhibitor, including , , and with of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
Targets
In vitro
BI-97C1 potently inhibits cell growth of human prostate cancer, lung cancer, and lymphoma cell lines with EC50 values of 0.13, 0.56, and 0.049 μM, respectively, and shows little cytotoxicity against baxbak cells. It is suggest that treatment with the combination regimen of mda-7/IL-24 and BI-97C1 induces autophagy that facilitates apoptosis in association with up-regulation of NOXA, accumulation of Bim, and activation of Bax and Bak.
In vivo
BI-97C1 displays in vivo efficacy in transgenic mice in which Bcl-2 is overexpressed in splenic B-cells and also demonstrates superior single-agent antitumor efficacy in a prostate cancer mouse xenograft model that depends on Mcl-1 for survival. Treatment with Ad.5/3- and BI-97C1 significantly inhibits the growth of human PC xenografts in nude mice and spontaneously induced PC in Hi-myc transgenic mice. Tumor growth inhibition correlats with increased TUNEL staining and decreased Ki-67 expression in both PC xenografts
and prostates of Hi-myc mice.
References
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