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.
For research use only. We do not sell to patients.
- CAS No.: 2763637-66-5
- Formula: C29H31ClN8O3
- Molecular Weight:575.06
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
|
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) |
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Cell Line
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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
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[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] |
Chemical Information
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CAS No. 2763637-66-5
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Molecular Weight 575.06
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Formula C29H31ClN8O3
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Pan S,et al. Structural Optimization and Structure-Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one Derivatives as A New Class of Potent Inhibitors of Pan-Trk and Their Drug-Resistant Mutants. J Med Chem. 2022 Feb 10;65(3):2035-2058. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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