BTX-1188 | GSPT1 and IKZF1/3 PROTAC | Probechem Biochemicals

Chemical Structure : BTX-1188

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BTX-1188 (Sontigidomide, BTX1188)

货号: PC-23063Not For Human Use, Lab Use Only.

Sontigidomide (BTX-1188) is a first-in-class dual degrader of GSPT1 and IKZF1/3 with DC50 of 0.2 nM, 1 nM and 1 nM for GSPT1, IKZF1 and IKZF3 respectively, in DOHH-2 (lymphoma) cells.

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生物&药学活性

Sontigidomide (BTX-1188) is a first-in-class dual degrader of GSPT1 and IKZF1/3 with DC50 of 0.2 nM, 1 nM and 1 nM for GSPT1, IKZF1 and IKZF3 respectively, in DOHH-2 (lymphoma) cells.
BTX-1188 potently inhibits AML and solid tumor cell proliferation.
Sontigidomide (BTX-1188) potently inhibits aCD3-stimulated and LPS-induced cytokine induction in human PBMCs.
BTX-1188 is cytotoxic in various cancer cell lines such as MYC-dependent and non-MYC dependent lines (IC50 range: 0.5-20 nM) and primary human AML patient samples (IC50 range: 0.4-1.5 nM), including relapsed/refractory-, cytarabine and Venetoclax-resistant samples.
BTX-1188 (25 mg/kg, i.p. QD) is highly efficacious in NCI H1155 (NSCLC) xenograft model in BALB/c nude mice.

物理化学性质&存储条件

分子量	513.47
分子式	C26H22F3N3O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-[[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-5-yl]methyl]-alpha-oxo-4-[1-(trifluoromethyl)cyclopropyl]benzeneacetamide

参考文献

1. Patent US20200369679 A1

2. Aparajita Hoskote Chourasia, et al. Meeting Abstract: 2022 ASCO Annual Meeting I

BTX-1188 (Sontigidomide, BTX1188)

生物&药学活性

物理化学性质&存储条件

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BTX-1188 (Sontigidomide, BTX1188)

生物&药学活性

物理化学性质&存储条件

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