| Identification | Back Directory | [Name]
BI-97C1 | [CAS]
1228108-65-3 | [Synonyms]
BI-97C1
Sabutoclax
BI-97C1 USP/EP/BP
BI-97C1;SABUTOCLAX
(1R)-1,1',6,6',7,7'-Hexahydroxy-3,3'-dimethyl-N5,N5'-bis[(2R)-2-phenylpropyl]-[2,2'-binaphthalene]-5,5'-dicarboxamide
[2,2'-Binaphthalene]-5,5'-dicarboxamide, 1,1',6,6',7,7'-hexahydroxy-3,3'-dimethyl-N5,N5'-bis[(2R)-2-phenylpropyl]-, (1R) | [Molecular Formula]
C42H40N2O8 | [MOL File]
1228108-65-3.mol | [Molecular Weight]
700.776 |
| Chemical Properties | Back Directory | [Melting point ]
>130°C (dec.) | [Boiling point ]
905.9±65.0 °C(Predicted) | [density ]
1.358±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer | [solubility ]
DMSO (Slightly), Ethyl Acetate (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
7.35±0.50(Predicted) | [color ]
Light Brown to Brown |
| Hazard Information | Back Directory | [Uses]
Sabutoclax(BI-97C1) 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. | [Biological Activity]
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]. | [in vivo]
Sabutoclax (1-5 mg/kg; i.p.; every two days in 18 D) reduces tumor growth in M2182-bearing athymic nude mice[1].
| Animal Model: | athymic nude mice with tumor xenografts from M2182 cells in s.c. | | Dosage: | 1 mg/kg, 3 mg/kg, 5 mg/kg | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Showed ihibiting tumor growth to about 60% of the tumor volume. |
| [IC 50]
Bcl-xL: 0.31 μM (IC50); BCL2: 0.32 μM (IC50); Mcl-1: 0.2 μM (IC50); Bfl-1: 0.62 μM (IC50) | [storage]
Store at -20°C | [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. |
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| Company Name: |
Energy Chemical
|
| Telephone: |
400-0056266 |
| Website: |
www.energy-chemical.com |
| Company Name: |
Wuhan Topule
|
| Telephone: |
+86-02787215551 19945035818 |
| Website: |
http://www.topule.com/ |
|