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felezonexor（SL-801）

  Cat. No.:  DC60243   Featured
Chemical Structure
1076235-04-5
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Field of application
Felezonexor, also known as CBS9106, SL-801, and BMS566419, is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences. CBS9106 inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression. Oral administration of CBS9106 significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1076235-04-5
Chemical Name: 1-[[6-Chloro-5-(trifluoromethyl)pyridin-2-yl]amino]-3-(3,3-dimethylbutoxymethyl)-4-methylpyrrole-2,5-dione
Synonyms: 1H-Pyrrole-2,5-dione, 1-[[6-chloro-5-(trifluoromethyl)-2-pyridinyl]amino]-3-[(3,3-dimethylbutoxy)methyl]-4-methyl-;PAW9EP9BXO;SB17170;1-((6-Chloro-5-(trifluoromethyl)-2-pyridinyl)amino)-3-((3,3-dimethylbutoxy)methyl)-4-methyl-1H-pyrrole-2,5-dione;1-[[6-Chloro-5-(trifluoromethyl)pyridin-2-yl]amino]-3-(3,3-dimethylbutoxymethyl)-4-methylpyrrole-2,5-dione
SMILES: ClC1=C(C(F)(F)F)C([H])=C([H])C(=N1)N([H])N1C(C(C([H])([H])[H])=C(C1=O)C([H])([H])OC([H])([H])C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O
Formula: C18H21ClF3N3O3
M.Wt: 419.8259
Purity: 98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Sakakibara K, et al. CBS9106 is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. Blood. 2011 Oct 6;118(14):3922-31.
Description: CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities[1].
Target: CRM1[1]
In Vivo: CBS9106 (31.25-62.5 mg/kg for 5 times weekly, 125 mg/kg for 3 times weekly; p.o.; 2 weeks) significantly suppresses tumor growth at dose levels of 62.5 or 125 mg/kg in mice bearing human MM xenograft models[1]. Animal Model: SCID mice with RPMI-8226 cells[1] Dosage: 31.25, 62.5, 125 mg/kg Administration: Oal administration; 5 times weekly (31.25 and 62.5 mg/kg), 3 times weekly (125 mg/kg); 2 weeks Result: Showed statistically significant tumor growth inhibition at dose levels of 62.5 mg/kg or 125 mg/kg.
In Vitro: CBS9106 (0.01-10 μM; 72 hours) sensitizes cells to radiation and to suppress the growth of a variety of cancer cell lines. The estimated IC50 values range from 22.3 or 35.6 nM in multiple myeloma (MM).1S or RPMI-8226 cells and from 3 to 278 nM in 60 other human cancer cell lines[1]. CBS9106 (1-400 nM; 24 hours) decreases CRM1 protein expression levels in a dose-dependent manner[1]. Cell Viability Assay[1] Cell Line: MM.1S cells, RPMI-8226 cells Concentration: 0.01, 0.1, 10 μM Incubation Time: 72 hours Result: Suppressed the growth of a variety of cancer cell lines and the estimated IC50 values ranged from 22.3 or 35.6 nM in MM.1S or RPMI-8226 cells. Western Blot Analysis[1] Cell Line: MM.1S cells Concentration: 1, 3, 6, 12, 25, 50, 100, 200, 400 nM Incubation Time: 24 hours Result: The level of CRM1 protein expression markedly reduced in a dose-dependent manner.
References: [1]. Sakakibara K, et al. CBS9106 is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. Blood. 2011 Oct 6;118(14):3922-31.
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2018-0101
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