| CAS NO: | 1403-36-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Molecular Weight (MW) | 710.87 |
|---|---|
| Formula | C31H30N6O6S4 |
| CAS No. | 1403-36-7 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 100 mg/mL (140.7 mM) |
| Water: <1 mg/mL | |
| Ethanol: 10 mg/mL (14.0 mM) | |
| Solubility (In vivo) | O=C1N(C)[C@]2(CO)C(N3[C@]1(SS2)C[C@@]4(N5C=C(C[C@]6(N(C)C7=O)SS[C@]7(CO)N(C)C6=O)C8 =C5C=CC=C8)[C@]3([H])NC9=C4C=CC=C9)=O |
| Synonyms | NSC289491, BRN0077366; Chetomin; CTM; NSC-289491; NSC 289491 |
| In Vitro | In vitro activity: HIF-1 (hypoxia-inducible factors 1) is transcription factor which respond to changes of cellular environment oxygen. Chetomin selectively inhibits HIF-1 activities through disruption of the interaction of HIF-1 with its transcriptional coactivator p300. HIF-1 inhibition by chetomin effectively reduces hypoxia-dependent transcription and radiosensitizes hypoxic HT 1080 human fibrosarcoma cells in vitro. Chetomin attenuates the hypoxia-induced radioresistance of malignant glioma cell lines U251MG (DMF10: 1.35 and 1.18) and U343MG (DMF10: 1.78 and 1.48). Targeting of HIF-1 using chetomin abolishes the differentiation-inhibitory effect of hypoxia-inducible factor-1α. Kinase Assay: Cell Assay: In RT-PCR and clonogenic survival experiments, chetomin is added in a concentration of 150 nM to fully supplemented medium four hours before treatment with hypoxia. HT 1080 cells are then transferred to the hypoxic workstation (0.1% O2, 12 h) or to the well-humidified incubator (12 hours) without changing medium. HT1080 cells are thus treated for 16 hours with chetomin (150 nM) prior to radiation treatment. |
|---|---|
| In Vivo | Administration of chetomin in combination with forskolin significantly suppresses malignant glioma growth in an in vivo xenograft model. Che-M(chetomin loaded micelles) dramatically inhibits embryonic angiogenesis, tumor-induced angiogenesis and tumor growth in zebrafish. In mouse model, Che-M suppresses tumor growth and prolongs the survival in the subcutaneous CT26 tumor model. |
| Animal model | Transgenic fish Tg(flk1:EGFP); Mouse model(BALB/c mice) |
| Formulation & Dosage | Chetomin was loaded in micelles; 1 mg/mL(for zebrafish); 2 mg/kg(for mouse); s.c. |
| References | BMC Cancer. 2007 Nov 13;7:213; Br J Haematol. 2008 May; 141(3): 325–334; Nanoscale. 2014 Oct 21;6(20):11940-52. |
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