TNIK-IN-3 是一种有效，选择性和具有口服活性的TNIK激酶抑制剂，IC50值为 0.026 μM。TNIK-IN-3 还可以抑制FLT4(IC50=0.030 μM)，FLT1(IC50=0.191 μM) 和DRAK1(IC50=0.411 μM)。TNIK-IN-3 具有结直肠癌(CRC)的研究潜力。
产品描述
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 colorectal cancer(CRC) research [1].
体外活性
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 HCT116 and DLD-1 cell migration[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]. 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.
体内活性
TNIK-IN-3 (compound 21k) (100-150 mg/kg; p.o. twice daily for 18 days) dose-dependently inhibits tumor growth[1]. 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.
Cas No.
2754265-25-1
分子式
C23H18FN3O2
分子量
387.41
储存和溶解度
DMSO:75.6mg/mL (195.1mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
