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Cat. No.: HY-151945

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TRK II-IN-1

TRK II-IN-1 is a potent type II TRK inhibitor, with IC₅₀s of 3.3, 6.4, 4.3 and 9.4 nM, for TRKA/B/C and TRKA^G667C, respectively. TRK II-IN-1 also inhibits FLT3, RET, and VEGFR2 with IC₅₀s of 1.3, 9.9, and 71.1 nM, respectively. TRK II-IN-1 can be used for the research of TRK driven cancers.

For research use only. We do not sell to patients.

CAS No.: 2904690-41-9
Formula: C₂₉H₃₁F₃N₈O
Molecular Weight:564.60

Storage:

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

Data Sheet (274 KB)

TRK II-IN-1 Chemical Structure

CAS No.: 2904690-41-9

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

TrkA

3.3 nM (IC₅₀)

TrkB

6.4 nM (IC₅₀)

TrkC

4.3 nM (IC₅₀)

TRKA^G667C

9.4 nM (IC₅₀)

FLT3

1.3 nM (IC₅₀)

RET

9.9 nM (IC₅₀)

VEGFR2

71.1 nM (IC₅₀)

All Trk Receptor Isoforms :

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	10.2 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696A mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696A mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	104.5 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	143.3 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	15.7 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	2.6 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	26.1 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	28.2 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G623E mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G623E mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	31 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G623R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G623R mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	44.7 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	6.1 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	6.6 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	85.9 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G696S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]
BaF3	IC₅₀	>2000 nM Compound: 12d	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36410169]

In Vitro

TRK II-IN-1 (compound 12d) (1 μM) demonstrates over 90% of kinase inhibition towards VEGFR2, RET, FLT3 and nearly 70% inhibition against Kit, CSF1R, DDR1 and DDR2^[1].
TRK II-IN-1 (72 h) inhibits Ba/F3-CD74-TRKA, Ba/F3-ETV6-TRKB and Ba/F3-ETV6-TRKC cells, with IC₅₀s of 26.1, 44.7 and 15.7 nM, respectively^[1].
TRK II-IN-1 (72 h) suppresses proliferation of a panel of Ba/F3 cells stably transformed with wild type, xDFG as well as solvent-front (SF) mutant TRK fusion proteins, with IC₅₀s ranging from 2.6 to 143.3 nM^[1].
TRK II-IN-1 (0.4-500 nM; 48 h) induces apoptosis of Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKA^G667C cells^[1].
TRK II-IN-1 (0.4-500 nM; 24 h) arrests cell cycle progression in the G0/G1 phase in Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKA^G667C cells^[1].
TRK II-IN-1 (0.8-500 nM; 6 h) suppresses the phosphorylation of TRKA, TRKA^G667C kinases, and their downstream AKT, ERK and PLCγ1 in a dose-dependent manner^[1].

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

Apoptosis Analysis^[1]

Cell Line:

Ba/ F3 stable cell lines expressing wild type and G667C mutant fusions
Concentration:

0.4, 2, 10, 50 nM for Ba/F3-CD74-TRKA cells; 4, 20, 100, 500 nM for Ba/F3-CD74-TRKA^G667C cells
Incubation Time:

48 hours
Result:

Notable apoptotic cells (18.74% in 100 nM and 35.65% in 500 nM) were observed in Ba/F3-CD74-TRKA cells.
Induced Ba/F3-CD74-TRKA^G667C cell apoptosis with 11.22% and 56.25% at the concentration of 10 nM and 50 nM, respectively.

Cell Cycle Analysis^[1]

Cell Line:

Ba/ F3 stable cell lines expressing wild type and G667C mutant fusions
Concentration:

0.4, 2, 10, 50 nM for Ba/F3-CD74-TRKA cells; 4, 20, 100, 500 nM for Ba/F3-CD74-TRKA^G667C cells
Incubation Time:

24 hours
Result:

Arrested cell cycle progression in the G0/G1 phase.

Western Blot Analysis^[1]

Cell Line:

Ba/ F3 stable cell lines expressing wild type and G667C mutant fusions
Concentration:

0.8, 4, 20, 100, 500 nM
Incubation Time:

6 hours
Result:

Inhibited the activation of TRKA and downstream signaling.

Chemical Information

CAS No. 2904690-41-9
Molecular Weight 564.60
Formula C₂₉H₃₁F₃N₈O
SMILES

CN1CCN(CC1)CC2=CC=C(C=C2C(F)(F)F)NC([C@@H]3CCN(C3)C4=NN5C(C6=NC=CC=C6)=CN=C5C=C4)=O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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)

References

[1]. Xiang S, et, al. Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114899. [Content Brief]

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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.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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TRK II-IN-1

All Trk Receptor Isoforms

All VEGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

TRK II-IN-1 Related Classifications

HY-151945 Related Classifications