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说明： Selective p300/CBP bromodomain inhibitor
化学名： (6S)-1-(3,4-Difluorophenyl)-6-[5-(3,5-dimethyl-4-isoxazolyl)-1-(trans-4-methoxycyclohexyl)-1H-benzimidazol-2-yl]-2-piperidinone
纯度： ≥98% (HPLC)
生物活性 for CCS 1477
CCS 1477 is a selective p300/CBP bromodomain inhibitor. CCS 1477 binds with high affinity to p300 and CBP (Kd values are 1.3 and 1.7 nM, respectively), and with 170/130-fold selectivity compared with BRD4 (Kd = 222 nM). In vitro, CCS 1477 inhibits the proliferation of OPM-2 multiple myeloma cells (GI50 = 5 nM). Also, CCS 1477 inhibits cell proliferation in prostate cancer cell lines and decreases AR- and C-MYC-regulated gene expression. In vivo, CCS 1477 significantly improves survival and reduces tumor size in MOLM16 AML and OPM2 myeloma tumors in subcutaneous xenograft models. CCS 1477 is orally bioavailable.
许可信息
Sold under license from CellCentric Ltd
技术数据 for CCS 1477
| 分子量 | 534.61 |
| 公式 | C30H32F2N4O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2222941-37-7 |
| PubChem ID | 134457551 |
| InChI Key | SKDNDJWEBPQKCS-CLHVYKLBSA-N |
| Smiles | O=C1N(C2=CC(F)=C(C=C2)F)[C@@H](CCC1)C3=NC4=CC(C5=C(C)ON=C5C)=CC=C4N3[C@@H]6CC[C@H](CC6)OC |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CCS 1477
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 53.46 | 100 | |
| ethanol | 53.46 | 100 |
制备储备液 for CCS 1477
以下数据基于产品分子量 534.61。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.87 mL | 9.35 mL | 18.71 mL |
| 5 mM | 0.37 mL | 1.87 mL | 3.74 mL |
| 10 mM | 0.19 mL | 0.94 mL | 1.87 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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产品说明书 for CCS 1477
参考文献 for CCS 1477
参考文献是支持产品生物活性的出版物。
Nicosia et al (2023) Therapeutic targeting of EP300/CBP by bromodomain inhibition in hematologic malignancies. Cancer Cell 41 2136 PMID: 37995682
Welti et al (2021) Targeting the p300/CBP axis in lethal prostate cancer. Cancer Discov. 11 1118 PMID: 33431496
If you know of a relevant reference for CCS 1477, please let us know.
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关键词: CCS 1477, CCS 1477 supplier, CCS1477, CCS-1477, p300/CBP, bromodomain, inhibitors, inhibition, inhibit, selective, AML, myeloma, prostate, cancer, in, vivo, orally, bioavailable, AR, Bromodomains, Histone, Acetyltransferases, 8892, Tocris Bioscience
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