| Identification | Back Directory | [Name]
SSTC3 | [CAS]
1242422-09-8 | [Synonyms]
SSTC3
Benzamide, 4-[[methyl[4-(trifluoromethyl)phenyl]amino]sulfonyl]-N-[4-(2-pyridinyl)-2-thiazolyl]- | [Molecular Formula]
C23H17F3N4O3S2 | [MDL Number]
MFCD32708506 | [MOL File]
1242422-09-8.mol | [Molecular Weight]
518.53 |
| Hazard Information | Back Directory | [Description]
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors. | [Uses]
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors[1]. | [in vivo]
SSTC3 can be maintained for 24 hours after treatment[1].
SSTC3 (25 mg/kg, ip once daily for 8-12 days) suppresses the growth of colorectal carcinoma in CD-1 mice[1].
SSTC3 (10 mg/kg, ip once daily for 1 month) inhibits the growth of Apc mutation-driven tumors[1].
| Animal Model: | Five-week-old Apcmin mice[1]. | | Dosage: | 10 mg/kg. | | Administration: | IP for 1 month. | | Result: | Inhibited the growth of Apc mutation-driven tumors. |
| Animal Model: | CD-1 mice. | | Dosage: | 25 mg/kg. | | Administration: | IP once daily for 8-12 days. | | Result: | Inhibited the growth of HCT116 xenografts.
Attenuated the growth of this metastatic CRC PDX and markedly reduced the cell density of residual cancer.
Reduced the expression of WNT biomarkers in this CRC PDX.
|
| [References]
[1] Li B, et al, Differential abundance of CK1α provides selectivity for pharmacological CK1α activators to target WNT-dependent tumors. Sci Signal. 2017 Jun 27;10(485). pii: eaak9916. DOI:10.1126/scisignal.aak9916 |
|
|