1792999-26-8
1792999-26-8 structure
- Name: NCB-0846
- Chemical Name: NCB-0846
- CAS Number: 1792999-26-8
- Molecular Formula: C21H21N5O2
- Molecular Weight: 375.432
- Catalog: Signaling Pathways MAPK/ERK Pathway MAP4K
- Create Date: 2018-05-26 13:33:49
- Modify Date: 2024-01-06 11:33:39
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NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
| Name | NCB-0846 |
|---|---|
| Synonyms | 4-[2-(3H-benzimidazol-5-ylamino)quinazolin-8-yl]oxycyclohexan-1-ol |
| Description | NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM. |
|---|---|
| Related Catalog | |
| Target |
Wnt TNIK:21 nM (IC50) |
| In Vitro | NCB-0846 has anti-Wnt activity. NCB-0846 binds to TNIK in an inactive conformation, and this binding mode seems to be essential for Wnt inhibition. NCB-0846 shows inhibitory activity against TNIK with an IC50 of 21 nM. NCB-0846 also inhibits FLT3, JAK3, PDGFRα, TRKA, CDK2/CycA2, and HGK. NCB-0846 induces faster migration of TCF4 phosphorylated by TNIK within a concentration range of 0.1-0.3 μM and completely inhibits the phosphorylation of TCF4 at a concentration of 3 μM. NCB-0846 inhibits HCT116 cell growth and shows much higher (-20-fold) inhibitory activity against colony formation by the same cells in soft agar[1]. |
| In Vivo | NCB-0846 suppresses the growth of tumors established by inoculating HCT116 cells into immunodeficient mice. The expression of Wnt-target genes (AXIN2, MYC and CCND1) in xenografts is reduced following the administration of NCB-0846. NCB-0846 induces an increase in the sub-G1 cell population. Cleavage of poly (ADP-ribose) polymerase 1 indicates the induction of apoptosis[1]. |
| Animal Admin | Mice: NCB-0846 is suspended in DMSO/polyethylene glycol#400/30% 2-hydroxypropyl-β-cyclodextrin solution (10:45:45v/v). Five million HCT116 cells suspended in medium containing 25% Matrigel are inoculated into the subcutaneous tissues of 9-week-old female BALB/c nude mice. Mice are randomized according to tumour volume (9 mice per group). NCB-0846 was administered daily by oral gavage at 0 (vehicle alone), 40 or 80 mg/kg (body weight) BID (bis in die) for 14 days[1]. |
| References |
| Molecular Formula | C21H21N5O2 |
|---|---|
| Molecular Weight | 375.432 |
| Exact Mass | 375.17 |
| Storage condition | -20℃ |