For research use only. Not for therapeutic Use.
DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC)[1].
DS89002333 (0.001, 0.01, 0.1, 1, 10 µM; 30 min) inhibits phosphorylation of CREB in a dose-dependent manner in NIH/3T3 cells (phosphorylation status of CREB as a marker of intracellular PRAKACA inhibitory activity)[1].
DS89002333 (12.5, 50 mg/kg; p.o.; twice daliy for 5 days) shows anti-tumor activity in an NIH/3T3-fusion allograft model[1].
DS89002333 (3, 30 mg/kg; p.o.; twice daliy for 22 days) shows significant anti-tumor activity in FL-HCC PDX xenograft model[1].
| Catalog Number | I042835 |
| CAS Number | 2832159-79-0 |
| Synonyms | N-[(3-chloro-4-fluorophenyl)-[(2S,4R)-4-hydroxypyrrolidin-2-yl]methyl]-1-fluoro-7-methoxyisoquinoline-6-carboxamide |
| Molecular Formula | C22H20ClF2N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H20ClF2N3O3/c1-31-19-9-14-11(4-5-26-21(14)25)6-15(19)22(30)28-20(18-8-13(29)10-27-18)12-2-3-17(24)16(23)7-12/h2-7,9,13,18,20,27,29H,8,10H2,1H3,(H,28,30)/t13-,18+,20?/m1/s1 |
| InChIKey | KALMTELCNYQBGB-BPAMGIGYSA-N |
| SMILES | COC1=C(C=C2C=CN=C(C2=C1)F)C(=O)NC(C3CC(CN3)O)C4=CC(=C(C=C4)F)Cl |
| Reference | [1]. Toyota A, et al. ovel protein kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor shows anti-tumor activity in a fibrolamellar hepatocellular carcinoma model. Biochem Biophys Res Commun. 2022 Sep 17;621:157-161. |
