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JNJ-47117096 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-47117096 hydrochloride图片
CAS NO:1610536-69-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品名称
MELK-T1 hydrochloride
产品介绍
JNJ-47117096 hydrochloride 是一种有效的,选择性的MELK抑制剂,IC50值为 23 nM;同时对Flt3的作用较强,IC50值为 18 nM。
生物活性

JNJ-47117096 hydrochloride is potent and selectiveMELKinhibitor, with anIC50of 23 nM, also effectively inhibitsFlt3, with anIC50of 18 nM.

IC50& Target

IC50: 23 nM (MELK), 18 nM (Flt3)[1]

体外研究
(In Vitro)

JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50of 23 nM, also effectively inhibits Flt3, with an IC50of 18 nM, and slighitly blocks CAMKIIδ, Mnk2, CAMKIIγ, and MLCK (IC50, 810 nM, 760 nM, 1000 nM, 1000 nM). JNJ-47117096 (MELK-T1) suppresses the proliferation of Flt3-driven Ba/F3 cell lines, with an IC50of 1.5 μM in the absence of IL-3, while no inhibitory activity is observed in the presence of IL-3. JNJ-47117096 does not inhibit the proliferation of Ba/F3 cell lines transfected with either FGFR1, FGFR3, or KDR, either in the presence or absence of IL-3[1]. JNJ-47117096 (MELK-T1, 10 μM) delays the progression of MCF-7 cells through S-phase. JNJ-47117096 inhibits MELK, and then exerts stalled replication forks and DNA double-strand breaks (DSBs). JNJ-47117096 activates the ATM-mediated DNA-damage response (DDR). JNJ-47117096 (3, 10 μM) results in a growth arrest and a senescent phenotype. Moreover, JNJ-47117096 induces a strong phosphorylation of p53, a prolonged up-regulation of p21 and a down-regulation of FOXM1 target genes[2].

分子量

398.89

性状

Solid

Formula

C21H23ClN4O2

CAS 号

1610536-69-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 250 mg/mL(626.74 mM)

H2O : 3.33 mg/mL(8.35 mM;ultrasonic and warming and heat to 60℃)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5070 mL12.5348 mL25.0696 mL
5 mM0.5014 mL2.5070 mL5.0139 mL
10 mM0.2507 mL1.2535 mL2.5070 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。