2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Trk Receptor
  4. 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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Trk-IN-20 Chemical Structure

Trk-IN-20 Chemical Structure

CAS No. : 2460924-63-2

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Trk-IN-20 Related Antibodies

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TrkA TrkB TrkC Trk

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Description

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[1].

IC50 & Target

TrkA

1.6 nM (IC50)

TrkB

2.9 nM (IC50)

TrkC

2.0 nM (IC50)

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 (Kd) 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.

Trk-IN-20 Related Antibodies

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) AUC0-∞ (μM.h) Cmax (μM) T1/2 (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
Molecular Weight

376.40

Formula

C22H18F2N4
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Trk-IN-20 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trk-IN-202460924-63-2Trk ReceptorTropomyosin related kinase receptor3-Vinylindazoletropomyosin receptor kinaseTrkneurotrophic receptor tyrosine kinase geneNTRKfusioninhibitorresistancemutationInhibitorinhibit

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