felezonexor（SL-801）|cas 1076235-04-5|DC Chemicals

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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