CCS 1477
Tocris Bioscience, part of Bio-Techne | Catalog # 8892
Selective p300/CBP bromodomain inhibitor
Key Product Details
Description
Selective p300/CBP bromodomain inhibitor
Product Description
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.Licensing Information
Sold under license from CellCentric LtdProduct Specifications
Molecular Weight
534.61
Formula
C30H32F2N4O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(6S)-1-(3,4-Difluorophenyl)-6-[5-(3,5-dimethyl-4-isoxazolyl)-1-(trans-4-methoxycyclohexyl)-1H-benzimidazol-2-yl]-2-piperidinone
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
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.46 | 100 | |
| Ethanol | 53.46 | 100 |
Preparing Stock Solutions
for CCS 1477
The following data is based on the product molecular weight 534.61
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Welti Targeting the p300/CBP axis in lethal prostate cancer. Cancer Discov. 2021 PMID: 33431496
- Nicosia Therapeutic targeting of EP300/CBP by bromodomain inhibition in hematologic malignancies. Cancer Cell 2023 PMID: 37995682
Product Specific Notices for CCS 1477
For research use only
Loading...
Loading...