Chemical Structure : BTX-1188
CAS No.:
2560577-69-5
BTX-1188
(Sontigidomide, BTX1188)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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513.47
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Formula
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C26H22F3N3O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-[[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-5-yl]methyl]-alpha-oxo-4-[1-(trifluoromethyl)cyclopropyl]benzeneacetamide
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References
1. Patent US20200369679 A1
2. Aparajita Hoskote Chourasia, et al. Meeting Abstract: 2022 ASCO Annual Meeting I
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