CCS 1477

Name: CCS 1477
Brand: Tocris Bioscience
SKU: 8892

Tocris Bioscience, part of Bio-Techne | Catalog # 8892

COA / SDS

Selective p300/CBP bromodomain inhibitor

Key Product Details

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)
Molecular Weight:	534.61

View Full Technical Details for CCS 1477

Technical Data
Citations

Biological Activity for CCS 1477

CCS 1477 is a selective p300/CBP bromodomain inhibitor. CCS 1477 binds with high affinity to p300 and CBP (K_d values are 1.3 and 1.7 nM, respectively), and with 170/130-fold selectivity compared with BRD4 (K_d = 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 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 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

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References for CCS 1477

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