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Chemical Structure : CCS1477
CAS No.: 2222941-37-7
Catalog No.: PC-38126Not For Human Use, Lab Use Only.
CCS1477 (Inobrodib) is an orally bioavailable, potent, and selective inhibitor of the p300/CBP bromodomain, binds to p300 and CBP with Kds of 1.3 and 1.7 nM respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $158 | In stock | |
| 25 mg | $298 | In stock | |
| 50 mg | $498 | In stock | |
| 100 mg | $788 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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CCS1477 (Inobrodib) is an orally bioavailable, potent, and selective inhibitor of the p300/CBP bromodomain, binds to p300 and CBP with Kds of 1.3 and 1.7 nM respectively.
CCS1477 (Inobrodib) displays > 170/130-fold selectivity compared with BRD4, CCS1477 binding to cellular histones in an in-cell BRET assay, with an IC50 of 19 nM for p300 and 1060 nM for BRD4.
CCS1477 (Inobrodib) has only minimal binding to BRD2, 3, 4, 9 and WDR9 (14-33% of control at 1 uM) in a bromoscan assay of 32 bromodomains.
CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases AR- and C-MYC-regulated gene expression.
CCS1477 has antitumor activity, regulating AR and C-MYC signaling in AR-SV-driven models.
CCS1477 modulates KLK3 blood levels and regulates CRPC biopsy biomarker expression.
| M.Wt | 535.636 | |
| Formula | C31H35F2N3O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(3R)-2-(3,4-difluorophenyl)-3-(5-(3,5-dimethyl-4,5-dihydroisoxazol-4-yl)-1-((1r,4R)-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)cyclohexan-1-one |
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1. Jonathan Welti, et al. Cancer Discov. 2021 May;11(5):1118-1137.
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