| CAS NO: | 390362-78-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 458.48 |
|---|---|
| Formula | C22H17F2N2.CH3O4S |
| CAS No. | 390362-78-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 91 mg/mL (198.5 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Other info | Chemical Name:
3,11-difluoro-6,8,13-trimethyl-8H-quinolino[4,3,2-kl]acridin-13-ium methyl sulfate InChi Key: VRWGYMXWYZBBGF-UHFFFAOYSA-M InChi Code: InChI=1S/C22H17F2N2.CH4O4S/c1-12-8-16-15-10-13(23)4-6-18(15)26(3)22-17-11-14(24)5-7-19(17)25(2)20(9-12)21(16)22;1-5-6(2,3)4/h4-11H,1-3H3;1H3,(H,2,3,4)/q+1;/p-1 SMILES Code: C[N+]4=C2C3=C(C=C(C)C=C3C5=C4C=CC(F)=C5)N(C)C1=CC=C(F)C=C12.COS(=O)([O-])=O |
| Synonyms | NSC714187; NSC 714187; NSC-714187; RHPS 4 methosulfate; RHPS-4; RHPS 4; RHPS4. |
| In Vitro | In vitro activity: RHPS4 triggers a rapid and potent DNA damage response at telomeres in human transformed fibroblasts and melanoma cells, characterized by the formation of several telomeric foci containing phosphorylated DNA damage response factors γ-H2AX, RAD17, and 53BP1. This is dependent on DNA repair enzyme ATR, correlated with delocalization of the protective telomeric DNA–binding protein POT1, and is antagonized by overexpression of POT1 or TRF2. Cell Assay: RHPS4, used at a concentration of 1 μM for various times, is added to the cells 24 hours after plating. Cell counts and viability (trypan blue dye exclusion) are determined in each experiment. Caffeine at 10 mM, a dose with no toxic effect on cell viability, is left in the medium for 24 hours. Bleomycin is used at a concentration of 30 mM for 30 minutes. Cell lines used: Human transformed BJ-EHLT fibroblasts and M14 melanoma cells |
|---|---|
| In Vivo | In mice, RHPS4 exerted its antitumor effect on xenografts of human tumor cells of different histotype by telomere injury and tumor cell apoptosis. Tumor inhibition was accompanied by a strong DNA damage response, and tumors overexpressing POT1 or TRF2 were resistant to RHPS4 treatment. |
| Animal model | CD-1 male nude (nu/nu) mice |
| Formulation & Dosage | Dissolved in saline; 15 mg/kg/d; i.v. injection |
| References | Br J Cancer. 2007 Apr 23;96(8):1223-33; J Clin Invest. 2007 Nov;117(11):3236-47. |
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