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MedKoo Cat#: 466270 | Name: CCT373566
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Description:

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

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
CCT373566
CAS#2378853-66-6

Theoretical Analysis

MedKoo Cat#: 466270

Name: CCT373566

CAS#: 2378853-66-6

Chemical Formula: C26H29ClF2N6O3

Exact Mass: 546.1958

Molecular Weight: 547.00

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 Quantity
1mg USD 150.00 Ready to Ship
5mg USD 550.00 Ready to Ship
10mg USD 950.00 Ready to Ship
25mg USD 1,650.00 Ready to Ship
50mg USD 2,950.00 Ready to Ship
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Related CAS #
No Data
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
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.

Recalculate based on batch purity %
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.
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.