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Sabutoclax

In stock
Catalog No.
A4199
pan-Bcl-2 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$145.00
In stock
50mg
$675.00
In stock

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Background

Sabutoclax is an inhibitor of pan-Bcl-2 family with IC50 values of 0.32, 0.31, 0.20 and 0.62 μM for Bcl-2, Bcl-xL, Mcl-1 and Bfl-1, respectively [1].

Sabutoclax is a derivative of apogossypolone. It showed a high binding affinity to Bcl-xL both in NMR binding assay and in ITC assay, with a Kd value of 0.11μM. Sabutoclax also showed better cell membrane permeability than other apogossypolone derivatives. In PC3 cells, sabutoclax inhibited cell growth with EC50 value of 0.13 μM. In human BP3 cell line, sabutoclax induced cell apoptosis with IC50 value of 0.049 μM. In mice bearing M2182 cancer xenografts, administration of sabutoclax significantly reduced the tumor size. At dose of 5 mg/kg, sabutoclax induced near complete tumor growth suppression [1].

References:
[1] Wei J, Stebbins J L, Kitada S, et al. BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. Journal of medicinal chemistry, 2010, 53(10): 4166-4176.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt700.78
Cas No.1228108-65-3
FormulaC42H40N2O8
Solubility≥205.6 mg/mL in DMSO, ≥98.2 mg/mL in EtOH with ultrasonic, <2.47 mg/mL in H2O
Chemical Name2,3,5-trihydroxy-7-methyl-N-[(2R)-2-phenylpropyl]-6-[1,6,7-trihydroxy-3-methyl-5-[[(2R)-2-phenylpropyl]carbamoyl]naphthalen-2-yl]naphthalene-1-carboxamide
SDFDownload SDF
Canonical SMILESCC1=C(C(=C2C=C(C(=C(C2=C1)C(=O)NCC(C)C3=CC=CC=C3)O)O)O)C4=C(C=C5C(=C4O)C=C(C(=C5C(=O)NCC(C)C6=CC=CC=C6)O)O)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Sabutoclax(BI-97C1) is a inhibitor of Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 values of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
Targets Bcl-xL Bcl-2 Mcl-1 Bfl-1    
IC50 0.31 μM 0.32 μM 0.20 μM 0.62 μM    

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