Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewCCS 1477 New
Description: Selective p300/CBP bromodomain inhibitor
Chemical Name: (6S)-1-(3,4-Difluorophenyl)-6-[5-(3,5-dimethyl-4-isoxazolyl)-1-(trans-4-methoxycyclohexyl)-1H-benzimidazol-2-yl]-2-piperidinone
Purity: ≥98% (HPLC)
Biological Activity 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.
Licensing Information
Sold under license from Cell Centric Ltd
Technical Data for CCS 1477
| M. Wt | 534.61 |
| Formula | C30H32F2N4O3 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CCS 1477
| 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 will 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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets for CCS 1477
References for CCS 1477
References are publications that support the biological activity of the product.
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.
View Related Products by Target
View Related Products by Product Action
Keywords: 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
Citations for CCS 1477
Citations are publications that use Tocris products.
Currently there are no citations for CCS 1477. Do you know of a great paper that uses CCS 1477 from Tocris? Please let us know.
Reviews for CCS 1477
There are currently no reviews for this product. Be the first to review CCS 1477 and earn rewards!
Have you used CCS 1477?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cell Research Product Guide
This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:
- Self-renewal and Maintenance
- Differentiation
- Reprogramming
- Organoid Generation
- GMP and Ancillary Material Grade Products
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.