For research use only. Not for therapeutic Use.
ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice[1].
ASR-490 (0-1.6 µM; 24 h, 48 h) reduces the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 µM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells)[1].
ASR-490 (750 nM in HCT116 cells and 1.2 µM in SW620 cells, 24 h) shows apoptotic cell death and upregulation of the proapoptotic markers Bax and cleaved PARP Expression; inhibits the capability of colorectal cancer cells[1].
ASR-490 (HCT116 cells; 750 nM in 24 h, 600 nM in 48 h) overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants[1].
ASR-490 (5 mg/kg; i.p.; thrice a week for 4 weeks) inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice[1].
| Catalog Number | I044024 |
| CAS Number | 2690312-67-3 |
| Synonyms | [(2R,6S,7S,9R,15R,16S)-15-[(1S)-1-[(2R)-5-(hydroxymethyl)-4-methyl-6-oxo-2,3-dihydropyran-2-yl]ethyl]-2,16-dimethyl-3-oxo-8-oxapentacyclo[9.7.0.02,7.07,9.012,16]octadec-4-en-6-yl] pyridine-2-carboxylate |
| Molecular Formula | C34H41NO7 |
| Purity | ≥95% |
| InChI | InChI=1S/C34H41NO7/c1-18-15-26(40-30(38)21(18)17-36)19(2)22-8-9-23-20-16-29-34(42-29)28(41-31(39)25-7-5-6-14-35-25)11-10-27(37)33(34,4)24(20)12-13-32(22,23)3/h5-7,10-11,14,19-20,22-24,26,28-29,36H,8-9,12-13,15-17H2,1-4H3/t19-,20?,22+,23?,24?,26+,28-,29+,32+,33-,34+/m0/s1 |
| InChIKey | VLOZRPFAQLWDLI-NRQJBLMBSA-N |
| SMILES | CC1=C(C(=O)OC(C1)C(C)C2CCC3C2(CCC4C3CC5C6(C4(C(=O)C=CC6OC(=O)C7=CC=CC=N7)C)O5)C)CO |
| Reference | [1]. Tyagi A, et al. ASR490, a Small Molecule, Overrides Aberrant Expression of Notch1 in Colorectal Cancer. Mol Cancer Ther. 2020; 19(12):2422-2431. |
