Art. -Nr.: HY-124596

CD161

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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.

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Reinheit: 99.90%
CAS. Nr.: 1627716-22-6
Formel: C₂₆H₂₁N₅O₂
Molecular Weight:435.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CD161 Chemical Structure

CAS. Nr.: 1627716-22-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BT-20	IC₅₀	1713 nM Compound: 31	Cytotoxicity against human BT20 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human BT20 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
BT-474	IC₅₀	434 nM Compound: 31	Cytotoxicity against human BT474 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human BT474 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
BT-549	IC₅₀	410 nM Compound: 31	Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
HBL-100	IC₅₀	>2000 nM Compound: 31	Cytotoxicity against human HBL100 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human HBL100 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
HCC1143	IC₅₀	>2000 nM Compound: 31	Cytotoxicity against human HCC1143 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human HCC1143 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
HCC1395	IC₅₀	1233 nM Compound: 31	Cytotoxicity against human HCC1395 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human HCC1395 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
HCC1937	IC₅₀	>2000 nM Compound: 31	Cytotoxicity against human HCC1937 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human HCC1937 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
HCC1954	IC₅₀	1604 nM Compound: 31	Cytotoxicity against human HCC1954 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human HCC1954 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
HCC38	IC₅₀	285 nM Compound: 31	Cytotoxicity against human HCC38 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human HCC38 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
HCC70	IC₅₀	1623 nM Compound: 31	Cytotoxicity against human HCC70 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human HCC70 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
MDA-MB-157	IC₅₀	39 nM Compound: 31	Cytotoxicity against human MDA-MB-157 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MDA-MB-157 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
MDA-MB-231	IC₅₀	244 nM Compound: 31	Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
MDA-MB-361	IC₅₀	189 nM Compound: 31	Cytotoxicity against human MDA-MB-361 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MDA-MB-361 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
MDA-MB-436	IC₅₀	1698 nM Compound: 31	Cytotoxicity against human MDA-MB-436 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MDA-MB-436 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
MDA-MB-453	IC₅₀	188 nM Compound: 31	Cytotoxicity against human MDA-MB-453 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MDA-MB-453 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
MDA-MB-468	IC₅₀	1018 nM Compound: 31	Cytotoxicity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
MOLM-13	IC₅₀	53 nM Compound: 31	Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay	[PMID: 28463487]
MV4-11	IC₅₀	26 nM Compound: 31	Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay	[PMID: 28463487]
SUM149PT	IC₅₀	601 nM Compound: 31	Cytotoxicity against human SUM149PT cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human SUM149PT cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]
SUM-159-PT	IC₅₀	>2000 nM Compound: 31	Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human SUM159PT cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28463487]

In Vitro

CD161 has K_is 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 (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 t_1/2 of 2.4 hours (iv) and 2.9 hours (po) for rat; the C_max of 7333 ng/mL (po) for rat. The t_1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the C_max of mice is 983.1 ng/mL (po) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 t_1/2 of rat is 2.4 hours (iv) and 2.9 hours (po); the C_maxof rat is 7333 ng/mL (po). The t_1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the C_max of mice is 983.1 ng/mL (po) ^[1].

Chemical Information

CAS. Nr. 1627716-22-6
Appearance Solid
Molecular Weight 435.48
Formel C₂₆H₂₁N₅O₂
Color Light yellow to green yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 5 mg/mL (11.48 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2963 mL

11.4816 mL

22.9632 mL

5 mM

0.4593 mL

2.2963 mL

4.5926 mL

10 mM

0.2296 mL

1.1482 mL

2.2963 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2963 mL	11.4816 mL	22.9632 mL	57.4079 mL
	5 mM	0.4593 mL	2.2963 mL	4.5926 mL	11.4816 mL
	10 mM	0.2296 mL	1.1482 mL	2.2963 mL	5.7408 mL

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CD161

Anti-Blood Cancer Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CD161

Anti-Blood Cancer Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CD161 Related Classifications

HY-124596 Related Classifications