Chemical Structure : T6I-29
CAS No.:
2824308-33-8
T6I-29
(Selective estrogen receptor modulator)
Catalog No.: PC-22503Not For Human Use, Lab Use Only.
T6I-29 is a novel isoquinoline-based selective estrogen receptor modulator (SERM), interacts with Y537S ERα ligand binding domain (LBD), exhibits anti-proliferative activities, downregulates target genes, and elicits anti-tumoral activities.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
T6I-29 is a novel isoquinoline-based selective estrogen receptor modulator (SERM), interacts with Y537S ERα ligand binding domain (LBD), exhibits anti-proliferative activities, downregulates target genes, and elicits anti-tumoral activities.
T6I-29 demonstrates significant anti-proliferative activities in Y537S ERα breast cancer cells.
T6I-29 inhibits WT and Y537S ERα-Coactivator binding.
T6I-29 uniquely downregulates DKK1 in Y537S ESR1 breast cancer cells.
The active enantiomer of T6I-29, T6I-29-1A (25 mg/kg) inhibits tumor growth in ESR1 MCF7 Y537S xenograft model.
Physicochemical Properties
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M.Wt
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514.64
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Formula
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C32H35FN2O3
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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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(1'-(4-((1-(3-fluoropropyl)pyrrolidin-3-yl)methoxy)phenyl)-6'-hydroxy-1',4'-dihydro-2'H-spiro[cyclopropane-1,3'-isoquinolin]-2'-yl)(phenyl)methanone
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References
1. Young KS, et al. bioRxiv [Preprint]. 2024 Jun 2:2024.05.28.596307.
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