製品番号: HY-156086

TRK-IN-24

TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA^G595R, TRKA^G667C and TRKA^F589L IC₅₀s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1^G595R and BaF3-CD74-NTRK1^G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC₅₀ of 1.43-47.56 nM.

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CAS 番号: 2937544-01-7
分子式: C₃₉H₄₅N₇O₃
分子量:659.82

保管条件:

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

Data Sheet (269 KB)

TRK-IN-24 構造式

CAS 番号: 2937544-01-7

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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
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

IC50: 5.21 nM (TRKA), 4.51 nM (TRKC), 6.77 nM (TRKA^G595R), 1.42 nM (TRKA^G667C), 6.13 nM (TRKA^F589L)^[1]

Trk Receptor 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
BaF3	IC₅₀	1.43 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.7 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	121.09 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	17.67 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.36 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.37 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.38 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.46 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	22.82 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	25.44 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	26.4 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	27.07 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	27.2 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	315.8 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	46.15 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	47.56 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.12 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.56 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	6.13 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	6.42 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	7.68 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	8.62 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	982.75 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method	[PMID: 37676745]

体外実験

TRK-IN-24 (compound 10g) (3.7-300 nM) inhibits the phosphorylation of AKT, TRKA, PLCγ1, and ERK in Ba/F3 cells^[1].

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

体内実験

TRK-IN-24 (compound 10g) (50 mg/kg; 10-14 days) in mice BaF3-CD74-NTRK1^G595R and BaF3-CD74-NTRK1^G667C In xenograft models, treatment resulted in 72% and 78% tumor regression after 10 or 14 days, respectively^[1].

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

化学情報

CAS 番号 2937544-01-7
分子量 659.82
分子式 C₃₉H₄₅N₇O₃
SMILES

CC(C(C#CC1=CN=C2C=CC3=NN21)=CC(OCCCCCCCNC3=O)=C4)=C4C(NC5=CC(C6CC6)=CC(CN7CCN(CC7)C)=C5)=O
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 (269 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]. Wang Z, et al. Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations. J Med Chem. 2023 Sep 7.. . [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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分子量分子量

希釈計算機

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濃度 _(終了) 濃度 _(終了)

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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.

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