76958-67-3
基本信息
Nsc354462
Hypothemicin
HYPOTHEMYCIN
Hypothemycin - CAS 76958-67-3 - Calbiochem
(1aR,3S,4S,6Z,9S,15bR)-1a,8,9,15b-Tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-3H-oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione
(1aR,3S,4S,6Z,9S,15bR)-1a,8,9,15b-Tetrahydro-3,4,12-trihydroxy-9-methyl-14-methoxy-3H-oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione
(1aR,3S,4S,6Z,9S,15bR)-1a,2,4,5,11,8,9,15b-Octahydro-3,4,12-trihydroxy-9-methyl-14-methoxy-3H-oxireno[k][2]benzoxacyclotetradecin-5,11-dione
3H-Oxireno[k][2]benzoxacyclotetradecin-5,11(2H,4H)-dione,1a,8,9,15b-tetrahydro-3,4,12-trihydroxy-14-methoxy-9-methyl-,(1aR,3S,4S,6Z,9S,15bR)-
物理化学性质
| 熔点 | 170-172℃ |
| 储存条件 | -20°C |
| 溶解度 | 可溶于DMSO |
| 形态 | 冻干固体 |
| 颜色 | 白色 |
| 稳定性 | 可在-20°C的DMSO中的溶液下储存长达3个月。 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302 |
| 防范说明 | P301+P312+P330 |
| 危险品标志 | Xn |
| 危险类别码 | 22 |
| WGK Germany | 3 |
| 海关编码 | 29419000 |
常见问题列表
|
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%. |