For research use only. Not for therapeutic Use.
PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity[1].
PHT-7.3 (200 mg/kg; i.p.; daily; for 20 days) exhibits cytostatic antitumor activity in the mut-KRas(G12S) A549 xenograft and mut-KRasG12V H441 xenograft[1].
| Catalog Number | I018979 |
| CAS Number | 1614225-93-2 |
| Synonyms | 4-(1,3-dioxan-2-ylmethyl)-2-[[4-(4-methylphenyl)-1,3-thiazol-2-yl]methyl]phthalazin-1-one |
| Molecular Formula | C24H23N3O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C24H23N3O3S/c1-16-7-9-17(10-8-16)21-15-31-22(25-21)14-27-24(28)19-6-3-2-5-18(19)20(26-27)13-23-29-11-4-12-30-23/h2-3,5-10,15,23H,4,11-14H2,1H3 |
| InChIKey | AFPMVLVIYVAFSP-UHFFFAOYSA-N |
| SMILES | CC1=CC=C(C=C1)C2=CSC(=N2)CN3C(=O)C4=CC=CC=C4C(=N3)CC5OCCCO5 |
| Reference | [1]. Indarte M, et al. An Inhibitor of the Pleckstrin Homology Domain of CNK1 Selectively Blocks the Growth of Mutant KRAS Cells and Tumors. Cancer Res. 2019 Jun 15;79(12):3100-3111. |
