CCT373566 | CAS#2378853-66-6 | BCL6 degrader

CCT373566
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 466270

CAS#: 2378853-66-6

Description: CCT373566 is a highly potent BCL6 degrader (IC50 =0.7 nM) suitable for sustained depletion of BCL6 in vivo. CCT373566 showed modest in vivo efficacy in a lymphoma xenograft mouse model following oral dosing. The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies.

Chemical Structure

CCT373566

CAS# 2378853-66-6

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 466270
Name: CCT373566
CAS#: 2378853-66-6
Chemical Formula: C26H29ClF2N6O3
Exact Mass: 546.20
Molecular Weight: 547.004
Elemental Analysis: C, 57.09; H, 5.34; Cl, 6.48; F, 6.95; N, 15.36; O, 8.77

Price and Availability

Size	Price	Availability
1mg	USD 150	Ready to Ship
5mg	USD 550	Ready to Ship
10mg	USD 950	Ready to Ship
25mg	USD 1650	Ready to Ship
50mg	USD 2950	Ready to Ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: CCT373566; CCT 373566; CCT-373566;

IUPAC/Chemical Name: (S)-10-((5-chloro-2-((3R,5S)-3-hydroxy-5-methylpiperidin-1-yl)pyrimidin-4-yl)amino)-2-cyclopropyl-3,3-difluoro-7-methyl-1,2,3,4-tetrahydro-[1,4]oxazepino[2,3-c]quinolin-6(7H)-one

InChi Key: GSGDUDAFETZSPM-IATAILRESA-N

InChi Code: InChI=1S/C26H29ClF2N6O3/c1-13-7-16(36)11-35(10-13)25-30-9-18(27)23(33-25)31-15-5-6-19-17(8-15)20-21(24(37)34(19)2)38-12-26(28,29)22(32-20)14-3-4-14/h5-6,8-9,13-14,16,22,32,36H,3-4,7,10-12H2,1-2H3,(H,30,31,33)/t13-,16+,22-/m0/s1

SMILES Code: CN(C1=C(C2=C3OCC(F)(F)[C@H](C4CC4)N2)C=C(NC5=NC(N6C[C@H](O)C[C@H](C)C6)=NC=C5Cl)C=C1)C3=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#Y23X01M18

QC Data:

View QC data: current batch, Lot#Y23X01M18

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	CCT373566 is a potent and orally active degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM.
In vitro activity:	The antiproliferative activity of the degrader CCT373566 and the inhibitor CCT373567 was tested in a panel of cell lines (Table 5). The degradation of BCL6 by CCT373566 translated into potent antiproliferative activity. Reference: J Med Chem. 2022 Jun 23;65(12):8191-8207. https://pubmed.ncbi.nlm.nih.gov/35653645/
In vivo activity:	CCT373566 showed modest in vivo efficacy in a lymphoma xenograft mouse model following oral dosing. Tumor concentrations of CCT373566 were lower than plasma concentrations at all time points consistent with the low Vss (0.47 L/kg) seen in the initial PK studies (Figure S4). Reference: J Med Chem. 2022 Jun 23;65(12):8191-8207. https://pubmed.ncbi.nlm.nih.gov/35653645/

Preparing Stock Solutions

The following data is based on the product molecular weight 547.00 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	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Huckvale R, Harnden AC, Cheung KJ, Pierrat OA, Talbot R, Box GM, Henley AT, de Haven Brandon AK, Hallsworth AE, Bright MD, Akpinar HA, Miller DSJ, Tarantino D, Gowan S, Hayes A, Gunnell EA, Brennan A, Davis OA, Johnson LD, de Klerk S, McAndrew C, Le Bihan YV, Meniconi M, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Bellenie BR, Hoelder S. Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo. J Med Chem. 2022 Jun 23;65(12):8191-8207. doi: 10.1021/acs.jmedchem.1c02175. Epub 2022 Jun 2. PMID: 35653645; PMCID: PMC9234961.
In vitro protocol:	1. Huckvale R, Harnden AC, Cheung KJ, Pierrat OA, Talbot R, Box GM, Henley AT, de Haven Brandon AK, Hallsworth AE, Bright MD, Akpinar HA, Miller DSJ, Tarantino D, Gowan S, Hayes A, Gunnell EA, Brennan A, Davis OA, Johnson LD, de Klerk S, McAndrew C, Le Bihan YV, Meniconi M, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Bellenie BR, Hoelder S. Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo. J Med Chem. 2022 Jun 23;65(12):8191-8207. doi: 10.1021/acs.jmedchem.1c02175. Epub 2022 Jun 2. PMID: 35653645; PMCID: PMC9234961.
In vivo protocol:	1. Huckvale R, Harnden AC, Cheung KJ, Pierrat OA, Talbot R, Box GM, Henley AT, de Haven Brandon AK, Hallsworth AE, Bright MD, Akpinar HA, Miller DSJ, Tarantino D, Gowan S, Hayes A, Gunnell EA, Brennan A, Davis OA, Johnson LD, de Klerk S, McAndrew C, Le Bihan YV, Meniconi M, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Bellenie BR, Hoelder S. Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo. J Med Chem. 2022 Jun 23;65(12):8191-8207. doi: 10.1021/acs.jmedchem.1c02175. Epub 2022 Jun 2. PMID: 35653645; PMCID: PMC9234961.

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

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1: Huckvale R, Harnden AC, Cheung KJ, Pierrat OA, Talbot R, Box GM, Henley AT, de Haven Brandon AK, Hallsworth AE, Bright MD, Akpinar HA, Miller DSJ, Tarantino D, Gowan S, Hayes A, Gunnell EA, Brennan A, Davis OA, Johnson LD, de Klerk S, McAndrew C, Le Bihan YV, Meniconi M, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Bellenie BR, Hoelder S. Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo. J Med Chem. 2022 Jun 23;65(12):8191-8207. doi: 10.1021/acs.jmedchem.1c02175. Epub 2022 Jun 2. PMID: 35653645.

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