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2096992-20-8

中文名稱 MELK8A HYDROCHLORIDE
英文名稱 MELK-8a (hydrochloride)
CAS 2096992-20-8
分子式 C??H??ClN?O
分子量 469.03
MOL 文件 2096992-20-8.mol
2096992-20-8 結(jié)構(gòu)式 2096992-20-8 結(jié)構(gòu)式

基本信息

中文別名
母體胚胎亮氨酸拉鏈激酶(MELK)抑制劑(MELK-8A HYDROCHLORIDE)
英文別名
MELK-8a (hydrochloride)
NVP-MELK8a hydrochloride
所屬類別
生物化工:亮氨酸類衍生物

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMF: insol; DMSO: insol; Ethanol: insol; PBS (pH 7.2): 1 mg/ml
形態(tài)固體
顏色Light yellow to yellow
MELK8A HYDROCHLORIDE價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-100368AMELK8A HYDROCHLORIDE
MELK-8a hydrochloride
2096992-20-81mg1500元
2024/11/08HY-100368AMELK8A HYDROCHLORIDE
MELK-8a hydrochloride
2096992-20-85mg2800元
2024/11/08HY-100368AMELK8A HYDROCHLORIDE
MELK-8a hydrochloride
2096992-20-810mM * 1mLin DMSO2889元

常見(jiàn)問(wèn)題列表

生物活性
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。
靶點(diǎn)

IC50: 2 nM (MELK)

體外研究

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.

體內(nèi)研究

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.

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