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Art. -Nr.: HY-150561

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Trk-IN-20

Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC₅₀ values of 1.6 nM, 2.9 nM and 2.0 nM, respectively.

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CAS. Nr.: 2460924-63-2
Formel: C₂₂H₁₈F₂N₄
Molecular Weight:376.40

Speicherung:

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

Data Sheet (285 KB)

Trk-IN-20 Chemical Structure

CAS. Nr.: 2460924-63-2

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

TrkA

1.6 nM (IC₅₀)

TrkB

2.9 nM (IC₅₀)

TrkC

2.0 nM (IC₅₀)

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.009 μM Compound: 7mb	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.015 μM Compound: 7mb	Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.018 μM Compound: 7mb	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G696A mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G696A mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.022 μM Compound: 7mb	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.031 μM Compound: 7mb	Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G667C mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G667C mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.144 μM Compound: 7mb	Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G595R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type CD74-NTRK1 (unknown origin) harbouring G595R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.243 μM Compound: 7mb	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G623R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK3 (unknown origin) harbouring G623R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	0.503 μM Compound: 7mb	Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) harbouring G639R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells transfected with wild type ETV6-NTRK2 (unknown origin) harbouring G639R mutation assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]
BaF3	IC₅₀	3.116 μM Compound: 7mb	Antiproliferative activity against mouse BaF3 cells assessed as cell viability measured after 72 hrs by Micro plate reader method Antiproliferative activity against mouse BaF3 cells assessed as cell viability measured after 72 hrs by Micro plate reader method	[PMID: 32702585]

In Vitro

NTRK1 is a proto-oncogene in colon cancer, Trk inhibitors have been detected to against a variety of human cancers^[1].
Trk-IN-20 (compound 7mb) (0.031, or 0.018 μM, respectively; 72 h) exhibits strong inhibition against the Larotrectinib-resistant cells with NTRK1-G667C or NTRK3-G696A mutations with IC₅₀s of 0.031 and 0.018 μM, respectively^[1].
Trk-IN-20 (compound 7mb) (9-22 nM; 72 h) inhibits BaF3 murine cells stably transformed with NTRK oncogenic fusions including CD74-NTRK1, ETV6-NTRK2 and ETV6-NTRK3 with IC₅₀s of 15, 22, and 9 nM, respectively^[1].
Trk-IN-20 (compound 7mb) (0.32, 1.6, 8, 40, 200; 6 h) inhibits activation of Trk and its downstream proteins in BaF3-CD74-NTRK1, BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells^[1].
Trk-IN-20 (compound 7mb) tightly bound to ATP-binding site of TrkA, TrkB, and TrkC with binding constant (K_d) values of 1.6, 3.1 and 4.9 nM, respectively^[1].

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

Western Blot Analysis^[1]

Cell Line:

BaF3-CD74-NTRK1, BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells
Concentration:

0, 0.32, 1.6, 8, 40, 200 nM
Incubation Time:

6 hours
Result:

Inhibited the phosphorylation of TrkA/B/C and their downstream signaling molecules ERK, AKT, and PLC-γ1. And also induced partial degradation of Trk protein in BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells.

In Vivo

Trk-IN-20 (compound 7mb) (p.o.; 10 mg/kg) shows short half-life of 1.39 hours and a low oral bioavailability of 8.79% in rats^[1].

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

Animal Model:

Pharmacokinetic Profile of Trk-IN-20 (Compound 7mb) in Rats^[1]
Dosage:
Administration:
Result:

Route Dose (mg/kg) AUC_0-∞ (μM.h) C_max (μM) T_1/2 (h) CL (L/h/kg) BA (%)

i.v. 2 3.69 6.77 1.39 1.44 /

p.o. 10 1.62 0.36 1.13 - 8.79

Chemical Information

CAS. Nr. 2460924-63-2
Molecular Weight 376.40
Formel C₂₂H₁₈F₂N₄
SMILES

FC1=CC([C@@H](C)NC2=CC3=C(C=C2)NN=C3/C=C/C4=NC=CC=C4)=CC(F)=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 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)
Handling Instructions (2659 KB)

Verweise

[1]. Duan Y, et al. Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors. Eur J Med Chem. 2020 Oct 1. 203:112552. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

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