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製品番号: HY-144690

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D5261

D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor.

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CAS 番号: 1574574-57-4
分子式: C₂₅H₂₉N₅O₃
分子量:447.53

保管条件:

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

Data Sheet (271 KB)

D5261 構造式

CAS 番号: 1574574-57-4

容量

価格（税別）

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数量

Amount: USD 0.00

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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
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

D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor^[1].

IC₅₀ & Target

TrkA

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	>10 μM Compound: D5261	Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34871843]
BaF3	IC₅₀	>10 μM Compound: D5261	Antiproliferative activity against mouse BaF3 cells expressing EML4 fused TRKC assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing EML4 fused TRKC assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34871843]
BaF3	IC₅₀	2.91 μM Compound: D5261	Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing CD74 fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34871843]
BaF3	IC₅₀	3.32 μM Compound: D5261	Antiproliferative activity against mouse BaF3 cells expressing MPRIP fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing MPRIP fused TRKA assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34871843]
BaF3	IC₅₀	6.17 μM Compound: D5261	Antiproliferative activity against mouse BaF3 cells expressing QKI fused TRKB assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing QKI fused TRKB assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 34871843]

体外実験

D5261 (0-10 µM, 72 h) displays favorable anti-proliferative activity in Ba/F3-MPRIP-TrkA cells (IC₅₀ = 3.32 µM) and Ba/F3 CD74-TrkA cells (IC₅₀ = 2.91 µM) ^[1].
D5261 exhibits cellular selectivity over TrkB/C to some extent (Ba/F3 IC₅₀ > 10 µM, Ba/F3-QKI-TrkB IC₅₀ = 6.17 µM and Ba/F3-EML4-TrkC IC₅₀ > 10 µM)^[1].
D5261 (0-50 µM) inhibits the TrkA autophosphorylation and downstream signaling in a concentration-dependent manner^[1].
D5261 shows inhibitory activity against Ba/F3 cells harboring TrkA mutants (G667C, G667S, G667A, G595R and V573 M)^[1].

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

Cell Viability Assay^[1]

Cell Line:

Ba/F3-MPRIP-TrkA, Ba/F3 CD74-TrkA cells
Concentration:

0-10 µM
Incubation Time:

72 h
Result:

Displayed favorable anti-proliferative activity with an IC₅₀ of 3.32 and 2.91 µM against Ba/F3-MPRIP-TrkA and Ba/F3 CD74-TrkA cells, respectively.

Western Blot Analysis^[1]

Cell Line:

Ba/F3 CD74-TrkA cells
Concentration:

0.08, 0.4, 2, 10, and 50 µM
Incubation Time:
Result:

Inhibited the TrkA autophosphorylation and phosphorylation of downstream PLCγ1, AKT and ERK in a concentration-dependent manner.

化学情報

CAS 番号 1574574-57-4
分子量 447.53
分子式 C₂₅H₂₉N₅O₃
SMILES

CC1=C(C=C(C=C1)C(NC2=CN=C(C=C2)N3CCN(C3=O)C4CCCC4)=O)N5CCCC5=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 (271 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]. Jing Guo, et al. Discovery of novel TrkA allosteric inhibitors: Structure-based virtual screening, biological evaluation and preliminary SAR studies. Eur J Med Chem. 2022 Jan 15;228:114022. [Content Brief]

Calculators

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)

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

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
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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D5261

Trk Receptor 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

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

D5261 関連分類

HY-144690 関連分類