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CD161 (Synonyms: NKR-P1A)

Cat. No.: HY-124596
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CD161 (NKR-P1A) 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.

For research use only. We do not sell to patients.

CD161 Chemical Structure

CD161 Chemical Structure

CAS No. : 1627716-22-6

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Description

CD161 (NKR-P1A) 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].

IC50 & Target

IC50: 28.2 nM (BRD4 BD1) and 7.2 nM (BRD4 BD2)[1]

In Vitro

CD161 (NKR-P1A) has Kis of 8.2 nM and 1.4 nM for BRD4 BD1 and BRD4 BD2, respectively[1].
CD161 (30-3000 nM; 1 hours) is very effective in inducing rapid down-regulation of c-Myc at as early as the 1 h time point and in a dose-dependent manner[1].

Western Blot Analysis[1]

Cell Line: MV4;11 leukemia cells.
Concentration: 30, 100, 300, 1000, 3000 nM
Incubation Time: 1 hours
Result: Induced rapid down-regulation of c-Myc at as early as the 1 hours time point and in a dose-dependent manner.
In Vivo

CD161 (NKR-P1A) (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.
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].
Molecular Weight

435.48

Formula

C₂₆H₂₁N₅O₂

CAS No.

1627716-22-6

SMILES

CC1=NC(C2=CC=NC3=CC=CC=C23)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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