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製品番号: HY-122653

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CCT367766

CCT367766 is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC₅₀ value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with K_d values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein.
(Pink: Pirin ligand (HY-184542); Blue: Cereblon ligand (HY-103596); Black: linker).

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CAS 番号: 2229856-58-8
分子式: C₄₉H₄₈ClN₇O₁₁
分子量:946.40

保管条件:

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

Data Sheet (267 KB)

CCT367766 構造式

CAS 番号: 2229856-58-8

容量

価格（税別）

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数量

Sample (0.1mg)

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(In Japan)

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Use of MCE Products

Fluorescent Dye

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

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製品説明

CCT367766 is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC₅₀ value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with K_d values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein^[1]. (Pink: Pirin ligand (HY-184542); Blue: Cereblon ligand (HY-103596); Black: linker).

IC₅₀ & Target^[1]

CRBN-DDB1

490 nM (IC₅₀)

PROTACs アイソフォーム固有の製品をすべて表示 :

体外実験

CCT367766 (50-1500 nM; 24 hours) demonstates the depletion of pirin protein as a the time-dependent hook-effect in SK-OV-3 human ovarian cancer cells^[1].
CCT367766 (0.5-50 nM; 2 hours) demonstrates the concentration-dependent depletion of pirin protein after 2 h exposure in SK-OV-3 cells^[1].
CCT367766 (0.5-50 nM; 2 hours) dose-dependently rescuses pirin expression from pretreatment of chlorobisamide in SK-OV-3 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

SK-OV-3 human ovarian cancer cells
Concentration:

50, 150, 250, 500 and 1500 nM
Incubation Time:

2 hours, 4 hours, 24 hours
Result:

Decreased pirin protein expression.

Western Blot Analysis^[1]

Cell Line:

SK-OV-3 human ovarian cancer cells
Concentration:

0.5, 1, 2.5, 5, 7.5, 10, 25, and 50 nM
Incubation Time:

2 hours
Result:

Completely degraded pirin just at 50 nM treatment.

化学情報

CAS 番号 2229856-58-8
分子量 946.40
分子式 C₄₉H₄₈ClN₇O₁₁
SMILES

O=C(C1=CC=C2N=C(CN3CCN(CCOCCOCCOC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)CC3)C=CC2=C1)NC7=CC(NC(C8=CC=C(OCCO9)C9=C8)=O)=CC=C7Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

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 (267 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]. Chessum NEA, et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).J Med Chem. 2018 Feb 8;61(3):918-933. [Content Brief]

Calculators

モル濃度計算機

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

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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.

Keywords

100 mg

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化学情報
純度とドキュメンテーション
参考文献

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