| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C29H31F3N8O |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
TRK II-IN-1 is a potent type II TRK inhibitor, with IC50 values of 3.3 nM, 6.4 nM, 4.3 nM, and 9.4 nM against TRKA, TRKB, TRKC, and the TRKA G667C mutant, respectively. It also inhibits FLT3, RET, and VEGFR2, with IC50 values of 1.3 nM, 9.9 nM, and 71.1 nM, respectively, and it can be used in the research of TRK-driven cancers[1]. Its molecular formula is C29H31F3N8O, with a molecular weight of 564.60 g/mol.
Physical & Chemical Properties
| CAS Number | 2904690-41-9 |
|---|---|
| Molecular Formula | C29H31F3N8O |
| Molecular Weight | 564.60 g/mol |
| 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 |
| Target | TrkA, TrkB, TrkC, TRKA G667C, FLT3, RET, VEGFR2 |
| Signaling Pathway | Neuronal Signaling; Protein Tyrosine Kinase/RTK |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
TrkA 3.3 nM (IC50) |
TrkB 6.4 nM (IC50) |
TrkC 4.3 nM (IC50) |
TRKAG667C 9.4 nM (IC50) |
FLT3 1.3 nM (IC50) |
RET 9.9 nM (IC50) |
VEGFR2 71.1 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
At 1 μM, TRK II-IN-1 inhibits the kinases VEGFR2, RET, and FLT3 by over 90% and Kit, CSF1R, DDR1, and DDR2 by nearly 70%[1]. Ba/F3-CD74-TRKA, Ba/F3-ETV6-TRKB and Ba/F3-ETV6-TRKC cells are inhibited by TRK II-IN-1 (72 h), with IC50s of 26.1, 44.7 and 15.7 nM, respectively[1]. Proliferation in a panel of Ba/F3 cells stably transformed with wild type, xDFG, or solvent-front (SF) mutant TRK fusion proteins is suppressed by TRK II-IN-1 (72 h), with IC50s ranging between 2.6 and 143.3 nM[1]. In Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells, TRK II-IN-1 (0.4-500 nM; 48 h) induces apoptosis[1]. At 0.4-500 nM for 24 h, TRK II-IN-1 arrests cell cycle progression of Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells in the G0/G1 phase[1]. At 0.8-500 nM for 6 h, TRK II-IN-1 dose-dependently suppresses phosphorylation of the TRKA and TRKAG667C kinases and of their downstream AKT, ERK and PLCγ1[1].
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-TRKAG667C 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-TRKAG667C 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-TRKAG667C 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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