country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-144690

Copy Link Print Information

D5261

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

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 1574574-57-4
Formule: C₂₅H₂₉N₅O₃
Masse moléculaire:447.53

Stockage:

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

Data Sheet (271 KB)

D5261 Chemical Structure

CAS No.: 1574574-57-4

Stock

Quantité

Amount: USD 0.00

* Veuillez sélectionner la quantité avant d'ajouter des articles.

Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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

IC₅₀ & Target

TrkA

Voir tous les produits spécifiques à Isoform Trk Receptor :

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]

In Vitro

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.

Chemical Information

CAS No. 1574574-57-4
Masse moléculaire 447.53
Formule C₂₅H₂₉N₅O₃
SMILES

CC1=C(C=C(C=C1)C(NC2=CN=C(C=C2)N3CCN(C3=O)C4CCCC4)=O)N5CCCC5=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 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)
Instruction de manipulation (2659 KB)

Références

[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

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Obtenir un devis En stock

Other size

Obtenir un devis