寄端霉素

生物活性靶点体外研究体内研究寄端霉素试剂级价格

寄端霉素

CAS号:76958-67-3
英文名:HYPOTHEMYCIN
中文名:寄端霉素
CBNumber:CB3229169
分子式:C19H22O8
分子量:378.37
MOL File:76958-67-3.mol

寄端霉素化学性质

熔点 :170-172℃
储存条件 :-20°C
溶解度 :DMSO: soluble
形态 :Lyophilized solid
颜色 :White
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

安全信息

危险品标志 :Xn
危险类别码 :22
WGK Germany :3
海关编码 :29419000

寄端霉素性质、用途与生产工艺

生物活性 Hypothemycin 是由真菌产生的聚酮化合物，是一种多激酶抑制剂，对 VEGFR2/VEGFR1，MEK1/MEK2，FLT-3，PDGFRβ/PDGFRα 和 ERK1/ERK2 的 Ki 值分别为 10/70 nM，17/38 nM, 90 nM，900 nM/1.5 μM 和 8.4/2.4 μM。

靶点

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)

体外研究

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.

体内研究

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%.