1. Neuronal Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. Trk Receptor Apoptosis
  3. Pan-Trk-IN-3

Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkAG595R, TrkAG667C, TrkAG667S, TrkAF589L and TrkCG623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis.

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Pan-Trk-IN-3

Pan-Trk-IN-3 Chemical Structure

CAS No. : 2763637-66-5

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Description

Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkAG595R, TrkAG667C, TrkAG667S, TrkAF589L and TrkCG623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis[1].

IC50 & Target

TrkA

2 nM (IC50)

TrkC

2 nM (IC50)

TrkB

3 nM (IC50)

TrkAG667S

5 nM (IC50)

TrkCG623R

6 nM (IC50)

TrkAF589L

7 nM (IC50)

TrkAG595R

21 nM (IC50)

TrkAG667C

26 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
BaF3 IC50
0.015 μM
Compound: 11g
Cytotoxicity against mouse BaF3 cells harboring TEL fused TrkC G613R mutant assessed as inhibition of cell growth by MTT assay
Cytotoxicity against mouse BaF3 cells harboring TEL fused TrkC G613R mutant assessed as inhibition of cell growth by MTT assay
[PMID: 35080890]
BaF3 IC50
0.5 nM
Compound: 11g
Cytotoxicity against mouse BaF3 cells expressing CD74 fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing CD74 fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
BaF3 IC50
1 nM
Compound: 11g
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667C mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667C mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
BaF3 IC50
1 nM
Compound: 11g
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkA assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
BaF3 IC50
12 nM
Compound: 11g
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G595R mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G595R mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
BaF3 IC50
13 nM
Compound: 11g
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
BaF3 IC50
15 nM
Compound: 11g
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G623R assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G623R assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
BaF3 IC50
2 nM
Compound: 11g
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G696C assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing TEL fused TrkC G696C assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
BaF3 IC50
6 nM
Compound: 11g
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667S mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA G667S mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
BaF3 IC50
7 nM
Compound: 11g
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA F589L mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing LMNA fused TrkA F589L mutant assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
BaF3 IC50
9526 nM
Compound: 11g
Cytotoxicity against mouse BaF3 assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
Cytotoxicity against mouse BaF3 assessed as inhibition of cell growth incubated for 3 days by CCK-8 assay
[PMID: 35080890]
Molecular Weight

575.06

Formula

C29H31ClN8O3

CAS No.
SMILES

CC1=CC(NC(NC2=CC(C(C)(C)C)=NN2C3=CC=C(C=C3)Cl)=O)=CC=C1NC4=C5OC(C)(C(NC5=NC=N4)=O)C

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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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

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Product Name:
Pan-Trk-IN-3
Cat. No.:
HY-144069
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