MELK8A HYDROCHLORIDE
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- CAS號:
- 2096992-20-8
- 英文名:
- MELK-8a (hydrochloride)
- 英文別名:
- MELK-8a (hydrochloride);NVP-MELK8a hydrochloride;1-Methyl-4-(4-(4-(3-(piperidin-4-ylmethoxy)pyridin-4-yl)-1H-pyrazol-1-yl)phenyl)piperazine hydrochloride;MELK-8a,inhibit,MELK,NVS-MELK8a,MELK8a hydrochloride,Maternal embryonic leucine zipper kinase,Inhibitor,MELK 8a hydrochloride
- 中文名:
- MELK8A HYDROCHLORIDE
- 中文別名:
- 鹽酸MELK-8A;化合物 T11996;化合物MELK-8A HYDROCHLORIDE;母體胚胎亮氨酸拉鏈激酶(MELK)抑制劑(MELK-8A HYDROCHLORIDE);1-甲基-4-(4-(4-(3-(哌啶-4-基甲氧基)吡啶-4-基)-1H-吡唑-1-基)苯基)哌嗪鹽酸鹽
- CBNumber:
- CB53167617
- 分子式:
- C25H33ClN6O
- 分子量:
- 469.03
- MOL File:
- 2096992-20-8.mol
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MELK8A HYDROCHLORIDE化學(xué)性質(zhì)
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儲存條件:
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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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形態(tài):
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A solid
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顏色:
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Light yellow to yellow
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MELK8A HYDROCHLORIDE性質(zhì)、用途與生產(chǎn)工藝
MELK-8a hydrochloride是一種新穎的母體胚胎亮氨酸拉鏈激酶（MELK）抑制劑，其IC50值為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
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS編號 | 包裝 | 價格 |
|---|
| 2024/11/08 | HY-100368A | MELK8A HYDROCHLORIDE
MELK-8a hydrochloride | 2096992-20-8 | 1mg | 1500元 |
| 2024/11/08 | HY-100368A | MELK8A HYDROCHLORIDE
MELK-8a hydrochloride | 2096992-20-8 | 5mg | 2800元 |
MELK8A HYDROCHLORIDE
生產(chǎn)廠家
2096992-20-8, MELK8A HYDROCHLORIDE 相關(guān)搜索:
- 抑制劑
- 藥靶配體
- 細(xì)胞生物學(xué)試劑
- 1-甲基-4-(4-(4-(3-(哌啶-4-基甲氧基)吡啶-4-基)-1H-吡唑-1-基)苯基)哌嗪鹽酸鹽
- 鹽酸MELK-8A
- 化合物MELK-8A HYDROCHLORIDE
- 化合物 T11996
- 母體胚胎亮氨酸拉鏈激酶(MELK)抑制劑(MELK-8A HYDROCHLORIDE)
- 2096992-20-8
- 1-Methyl-4-(4-(4-(3-(piperidin-4-ylmethoxy)pyridin-4-yl)-1H-pyrazol-1-yl)phenyl)piperazine hydrochloride
- MELK-8a,inhibit,MELK,NVS-MELK8a,MELK8a hydrochloride,Maternal embryonic leucine zipper kinase,Inhibitor,MELK 8a hydrochloride
- NVP-MELK8a hydrochloride
- MELK-8a (hydrochloride)