Chemical Structure : VPC-260724
CAS No.:
VPC-260724
(VPC260724)
Catalog No.: PC-23562Not For Human Use, Lab Use Only.
VPC-260724 is a specific small molecule inhibitor of estrogen receptor-activation function 2 (ER-AF2) with IC50 of 5.7 uM for inhibition of ER transcription in T47D-KBluc cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
VPC-260724 is a specific small molecule inhibitor of estrogen receptor-activation function 2 (ER-AF2) with IC50 of 5.7 uM for inhibition of ER transcription in T47D-KBluc cells.
VPC-260724 reduces viability in ER-positive T47D and MCF7, the ER-positive and tamoxifen-resistant TamR3 cell line with IC50 of 7.4 uM.
VPC-260724 does not significantly impact the transcriptional activities of AR, GR, or PR
VPC-260724 (10 uM, 48 h) significantly reduced ER-SRC3 interactions in both MCF7 and TamR3 cells.
VPC-260724 inhibits the growth of MCF7, and TamR3 spheroids with IC50 values of 15.6 ± 1.4 µM and 27.0 ± 3.2 µM, respectively.
VPC-260724 shows antiproliferative activity in ER-positive breast cancer models.
Physicochemical Properties
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M.Wt
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295.39
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Formula
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C17H21N5
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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,N-dimethyl-6-((((8-methylimidazo[1,2-a]pyridin-3-yl)methyl)amino)methyl)pyridin-2-amine
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References
1. Foo J, et al. Breast Cancer Res. 2024 Nov 26;26(1):168.
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