寄端霉素
寄端霉素 用途与合成方法
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VEGFR2 10 nM (Ki) |
VEGFR1 70 nM (Ki) |
MEK1 17 nM (Ki) |
MEK2 38 nM (Ki) |
FLT-3 90 nM (Ki) |
PDGFRα 1.5 μM (Ki) |
PDGFRβ 900 nM (Ki) |
ERK1 8.4 μM (Ki) |
ERK2 2.4 μM (Ki) |
Hypothemycin inhibits eosinophilic EOL1 cell carrying mutations in FIP1L1-PDGFRα, acute myeloid leukemia MV-4-11 cell carrying mutations in FLT3-ITD, melanoma COLO829 cell carrying mutations in BRAF V600E, HUVEC cell carrying mutations in VEGFR, mastocytoma P815 cell carrying mutations in c-KIT D814Y, NSCLC A459 cell carrying mutations in KRAS, and ovarian SKOV-3 cell carrying mutations in HER2 with IC 50 s of 0.4 nM, 6 nM, 50 nM, 70 nM, 370 nM, 6.0 μM, and 7.0 μM, respectively.
Hypothemycin (10 mg/kg) kills T. brucei in infected mice, completely curing the infection in one third of animals, although high doses of Hypothemycin (>10 mg/kg) leads to side effects.
| Animal Model: | Adult female Balb/c mice (weighing 18–22 g) infected with T. brucei |
| Dosage: | 10 mg/kg |
| Administration: | Administered once daily via intraperitoneal injection for 7 days. |
| Result: |
Showed a dose-dependent reduction in parasitemia in infected mice.
Prolonged survival of infected mice over 30 days, with a cure rate of 33%. |
