| Identification | Back Directory | [Name]
Cd161 | [CAS]
1627716-22-6 | [Synonyms]
Cd161
NKR-P1A
9H-Pyrimido[4,5-b]indole, 7-(3,5-dimethyl-4-isoxazolyl)-6-methoxy-2-methyl-4-(4-quinolinyl)- | [Molecular Formula]
C26H21N5O2 | [MDL Number]
MFCD32201066 | [MOL File]
1627716-22-6.mol | [Molecular Weight]
435.48 |
| Hazard Information | Back Directory | [Description]
CD-161 is a potent and orally bioavailable BET inhibitor. CD-161 has excellent microsomal stability and good oral pharmacokinetics in rats and mice. Orally administered, CD-161 achieves significant antitumor activity in the MV4-11 leukemia and MDA-MB-231 triple-negative breast cancer xenograft models in mice. | [Uses]
CD161 is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity[1]. | [in vivo]
CD161 (po; 20, 40 mg/kg/day; 45 days) achieves essentially complete tumor growth inhibition[1].
CD161 (5 mg/kg (iv), 25 mg/kg (po); 0-24 hours) has the t1/2 of 2.4 hours (iv) and 2.9 hours (po) for rat; the Cmax of 7333 ng/mL (po) for rat. The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) [1].
| Animal Model: | Dorsal side of severe combined immunodeficient (SCID) mice[1] | | Dosage: | 20, 40 mg/kg | | Administration: | Po; daily; 45 days | | Result: | Achieved essentially complete tumor growth inhibition.
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| Animal Model: | Rat or mice[1] | | Dosage: | 5 mg/kg (iv), 25 mg/kg (po) for rat and mice (Pharmacokinetic Study) | | Administration: | Iv and po; 0, 5, 15, 30 mins, and 1, 2, 4, 6, 8, 24 hours | | Result: | The t1/2 of rat is 2.4 hours (iv) and 2.9 hours (po); the Cmaxof rat is 7333 ng/mL (po). The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) [1].
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| [References]
[1] Zhao Y, et al. Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor. J Med Chem. 2017 May 11;60(9):3887-3901. DOI:10.1021/acs.jmedchem.7b00193 |
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| Company Name: |
BOC Sciences
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1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
ZSGB-BIO
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02-400-810-9781 400810978 |
| Website: |
www.zsbio.com |
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