[CAS NO. 2754265-25-1] TNIK-IN-3
PRODUCTS SPECIFICATIONS [2754265-25-1]
DESCRIPTION [2754265-25-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 387.41 |
| Molecular Formula | C23H18FN3O2 |
| SMILES | O=C1C2=CC=C(C=C2OCCN1CC3=CC=C(C=C3)F)C4=CC5=C(NC=C5)N=C4 |
Summary
TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK) , with an IC 50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 ( IC 50 =0.030 μM), Flt1 ( IC 50 =0.191 μM) and DRAK1 ( IC 50 =0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer [1] .
IC50 & Target
In Vitro
TNIK-IN-3 (compound 21k) inhibits Aurora-A, GCK, and MLK3 with IC
50
s of 0.517 μM, 3.657 μM, and 4.552 μM, respectively
[1]
.
TNIK-IN-3 (0.1-100 μM; 3 days) inhibits the viability of HCT116 and DLD-1 cells, with IC
50
s of 4.26 μM and 8.00 μM, respectively
[1]
.
TNIK-IN-3 (2.5-40 μM; 10 days) dose-dependently inhibits the colony formation of HCT116 and DLD-1 cells
[1]
.
TNIK-IN-3 (5-20 μM; 48 h) inhibits the migration of HCT116 and DLD-1 cells
[1]
.
TNIK-IN-3 (5-40 μM; 48 h) dose-dependently inhibits the expression ofLRP5 and LRP6 proteins, Wnt target genes AXIN2 and c-Myc in HCT116 cells
[1]
.
TNIK-IN-3 (5-20 μM; 48 h) significantly suppresses the phosphorylation of JNK1/2 in Hela cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | HCT116 and DLD-1 cells |
| Concentration: | 0.1-100 μM |
| Incubation Time: | 3 days |
| Result: | Inhibited cell viability in a dose-dependent manner. |
Cell Viability Assay [1]
| Cell Line: | HCT116 cells |
| Concentration: | 5, 10, 20, 40 μM |
| Incubation Time: | 48 hours |
| Result: | Inhibited the expression of Wnt target genes AXIN2 and c-Myc, LRP5 and LRP6 proteins. |
In Vivo
TNIK-IN-3 (compound 21k) (100-150 mg/kg; p.o. twice daily for 18 days) inhibits tumor growth in a dose-dependent manner
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Six-week-old female NOD-SCID mice were injected with HCT116 cells [1] |
| Dosage: | 100, 150 mg/kg |
| Administration: | P.o. twice daily for 18 days |
| Result: |
Significantly inhibited tumor growth at a dose of 150 mg/kg.
No obvious weight loss and no other side effects were observed. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 83.33 mg/mL ( 215.10 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5812 mL | 12.9062 mL | 25.8124 mL |
| 5 mM | 0.5162 mL | 2.5812 mL | 5.1625 mL |
| 10 mM | 0.2581 mL | 1.2906 mL | 2.5812 mL |