MELK8A HYDROCHLORIDE
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- CAS号:
- 2096992-20-8
- 英文名:
- MELK-8a (hydrochloride)
- 英文别名:
- MELK-8a (hydrochloride);NVP-MELK8a hydrochloride;MELK-8a,inhibit,MELK,NVS-MELK8a,MELK8a hydrochloride,Maternal embryonic leucine zipper kinase,Inhibitor,MELK 8a hydrochloride
- 中文名:
- MELK8A HYDROCHLORIDE
- 中文别名:
- 盐酸MELK-8A;化合物 T11996;化合物MELK-8A HYDROCHLORIDE;母体胚胎亮氨酸拉链激酶(MELK)抑制剂(MELK-8A HYDROCHLORIDE)
- CBNumber:
- CB53167617
- 分子式:
- C25H33ClN6O
- 分子量:
- 469.03
- MOL File:
- 2096992-20-8.mol
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MELK8A HYDROCHLORIDE化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMF: insol; DMSO: insol; Ethanol: insol; PBS (pH 7.2): 1 mg/ml
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形态:
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A solid
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MELK8A HYDROCHLORIDE性质、用途与生产工艺
MELK-8a hydrochloride是一种新颖的母体胚胎亮氨酸拉链激酶(MELK)抑制剂,其IC50值为2 nM。
MELK-8a remains very potent (IC
50
=140 nM) when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. Its potency is well tracked between full-length MELK versus catalytic domain construct (5 nM versus 2 nM). It only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. The compound is at least 90-fold more selective in targeting MELK in all cases. MELK-8a is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay. MELK-8a inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC
50
of approximately 0.06 and 1.2 μM, respectively.
Subcutaneous administration of MELK-8a at 30 mg/kg in C57BL/6 mice results in good plasma exposure. The compound adsorption into the systemic circulation is rapid (T
max
=0.4 h) and peak plasma concentration reaches 6.6 μM. An ascending dose PK study in female athymic nude mice shows that the rate of compound release is maximal at 120 mg/kg and all clearance mechanisms can be saturated at 240 mg/kg. However, when administered orally at 10 mg/kg in C57BL/6 male mice, it shows very poor PK (3.6% oral bioavailability) consistent with very high
in vivo
clearance.
MELK8A HYDROCHLORIDE
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/01/25 | HY-100368A | MELK8A HYDROCHLORIDE MELK-8a hydrochloride | 2096992-20-8 | 1mg | 1500元 |
2024/01/25 | HY-100368A | MELK8A HYDROCHLORIDE MELK-8a hydrochloride | 2096992-20-8 | 5mg | 3500元 |
MELK8A HYDROCHLORIDE
生产厂家
2096992-20-8, MELK8A HYDROCHLORIDE 相关搜索:
- 药靶配体
- 细胞生物学试剂
- 盐酸MELK-8A
- 化合物MELK-8A HYDROCHLORIDE
- 化合物 T11996
- 母体胚胎亮氨酸拉链激酶(MELK)抑制剂(MELK-8A HYDROCHLORIDE)
- 2096992-20-8
- MELK-8a,inhibit,MELK,NVS-MELK8a,MELK8a hydrochloride,Maternal embryonic leucine zipper kinase,Inhibitor,MELK 8a hydrochloride
- NVP-MELK8a hydrochloride
- MELK-8a (hydrochloride)