製品番号: HY-124596

CD161

Name: CD161
Brand: MedChemExpress
SKU: HY-124596
Price: 280.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.90%
CAS 番号: 1627716-22-6
分子式: C₂₆H₂₁N₅O₂
分子量:435.48

保管条件:

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

CD161 構造式

CAS 番号: 1627716-22-6

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

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

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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].

化学情報

CAS 番号 1627716-22-6
性状 Solid
分子量 435.48
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (282 KB)
SDS (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

CD161 関連分類

HY-124596 関連分類

Bioz