MELK-T1(JNJ-47117096) HCl

Product Name: MELK-T1(JNJ-47117096) HCl
CAS No.: 1610536-69-0
Chemical Name: MELK-T1(JNJ-47117096) HCl
Synonyms: MELK-T1 HCl;MELK-T1 HCl salt;JNJ-47117096 hcl;MELK-T1 HYDROCHLORIDE;MELK-T1(JNJ-47117096) HCl;JNJ-47117096 hydrochloride;JNJ 47117096 hydrochloride,JNJ47117096 hydrochloride;2-Methoxy-4-(1H-pyrazol-4-yl)-N-(2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)benzamide hydrochloride
CBNumber: CB23374494
Molecular Formula: C21H23ClN4O2
Formula Weight: 398.89
MOL File: 1610536-69-0.mol

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MELK-T1(JNJ-47117096) HCl Property

storage temp.: Store at -20°C
solubility: DMSO : ≥ 250 mg/mL (626.74 mM)
form: Solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0011272
Product name: JNJ-47117096hydrochloride
Purity: 99.40%
Packaging: 5mg
Price: $330
Updated: 2021/12/16

ChemScene

Product number: CS-0011272
Product name: JNJ-47117096hydrochloride
Purity: 99.40%
Packaging: 10mg
Price: $500
Updated: 2021/12/16

ChemScene

Product number: CS-0011272
Product name: JNJ-47117096hydrochloride
Purity: 99.40%
Packaging: 25mg
Price: $1100
Updated: 2021/12/16

ChemScene

Product number: CS-0011272
Product name: JNJ-47117096hydrochloride
Purity: 99.40%
Packaging: 50mg
Price: $1700
Updated: 2021/12/16

ChemScene

Product number: CS-0011272
Product name: JNJ-47117096hydrochloride
Purity: 99.40%
Packaging: 100mg
Price: $2700
Updated: 2021/12/16

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MELK-T1(JNJ-47117096) HCl Chemical Properties,Usage,Production

Uses

JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.

Biological Activity

MELK-T1(JNJ-47117096) HCl is a potent and selective MELK inhibitor with IC50 value of 23 nM; it also has strong effect on Flt3 with IC50 value of 18 nM.

in vitro

MELK-T1(JNJ-47117096) HCl is potent and selective MELK inhibitor, with an IC ₅₀ of 23 nM, also effectively inhibits Flt3, with an IC ₅₀ of 18 nM, and slighitly blocks CAMKIIδ, Mnk2, CAMKIIγ, and MLCK (IC ₅₀ , 810 nM, 760 nM, 1000 nM, 1000 nM). It suppresses the proliferation of Flt3 -driven Ba/F3 cell lines, with an IC ₅₀ of 1.5 μM in the absence of IL-3, while no inhibitory activity is observed in the presence of IL-3. It 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. 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.

target

IC50: 23 nM (MELK), 18 nM (Flt3)

References

[1] Johnson CN, et al. Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase. ACS Med Chem Lett. 2014 May 23;6(1):25-30. DOI:10.1021/ml5001245
[2] Beke L, et al. MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells. Biosci Rep. 2015 Oct 2;35(6). pii: e00267. DOI:10.1042/BSR20150194

MELK-T1(JNJ-47117096) HCl Preparation Products And Raw materials

Raw materials

Preparation Products

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MELK-T1(JNJ-47117096) HCl Suppliers

China 23 United States 4 Global 27

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
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Amadis Chemical Company Limited

Tel: 571-89925085
Fax: 0086-571-89925065
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TargetMol Chemicals Inc.

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Country: United States
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HANGZHOU CLAP TECHNOLOGY CO.,LTD

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Country: CHINA
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Wuxi Donghe Pharmaceutical Technology Co., Ltd.

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ChemeGen(Shanghai) Biotechnology Co.,Ltd.

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Country: China
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Shanghai hongqu biomedical technology co. LTD

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ShangHai ChuanQian Chemcial Technique Centre

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Beijing Jin Ming Biotechnology Co., Ltd.

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1610536-69-0, MELK-T1(JNJ-47117096) HClRelated Search:

MELK-T1(JNJ-47117096) HCl

JNJ-47117096 hydrochloride

MELK-T1 HCl

MELK-T1 HYDROCHLORIDE

JNJ-47117096 hcl

JNJ 47117096 hydrochloride,JNJ47117096 hydrochloride

MELK-T1 HCl salt

2-Methoxy-4-(1H-pyrazol-4-yl)-N-(2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)benzamide hydrochloride

1610536-69-0