| Company Name: |
ShangHai ChuanQian Chemcial Technique Centre
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| Tel: |
15869524721 |
| Email: |
3525679403@qq.com |
| Products Intro: |
Product Name:GSK3368715 (hydrochloride)
CAS:2227587-25-7
Purity:98% HPLC Package:5MG;10MG;50MG;100MG,1G,5G,10G
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| Company Name: |
Shanghai Yifei Biotechnology Co. , Ltd.
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| Tel: |
021-65675885 18964387627 |
| Email: |
customer_service@efebio.com |
| Products Intro: |
Product Name:GSK3368715 (hydrochloride)
CAS:2227587-25-7
Purity:98% Package:1mg;5mg;10mg
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| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:GSK3368715 hydrochloride
CAS:2227587-25-7
Package:50mg;10mg
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| Company Name: |
Cayman Chemical Company
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| Tel: |
800-364-9897 |
| Email: |
sales@caymanchem.com |
| Products Intro: |
Product Name:GSK3368715 (hydrochloride)
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| Company Name: |
Ningbo Chaoming Biotechnology Co., Ltd
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| Tel: |
13301662590 |
| Email: |
mandy@atkchemical.com |
| Products Intro: |
Product Name:1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-, hydrochloride (1:1)
CAS:2227587-25-7
Purity:95% Package:1G;5G;10G;50G;100G;1KG
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| | 1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-, hydrochloride (1:1) Basic information |
| Product Name: | 1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-, hydrochloride (1:1) | | Synonyms: | 1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-, hydrochloride (1:1);GSK3368715 (hydrochloride) | | CAS: | 2227587-25-7 | | MF: | C20H39ClN4O2 | | MW: | 403.01 | | EINECS: | | | Product Categories: | | | Mol File: | 2227587-25-7.mol | ![1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-, hydrochloride (1:1) Structure](CAS/20211123/GIF/2227587-25-7.gif) |
| | 1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-, hydrochloride (1:1) Chemical Properties |
| storage temp. | -20°C | | solubility | DMSO: 40 mg/ml | | form | A solid |
| | 1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-, hydrochloride (1:1) Usage And Synthesis |
| Uses | GSK3368715 (EPZ019997) hydrochloride is an orally active, reversible, SAM-noncompetitive type I protein arginine methyltransferase (PRMT) inhibitor with IC50 values of 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), and 1.7 nM (PRMT8). GSK3368715 hydrochloride induces a shift in arginine methylation states, alters exon usage, and exhibits potent anticancer activity[1]. | | Biological Activity | GSK3368715 is an inhibitor of type I protein arginine methyltransferases (PRMTs; IC50s = 3.1, 162, 38, 4.7, and 39 nM for PRMT1, 3, 4, 6, and 8, respectively).1 It is selective for type I PRMTs over PRMT5, 7, and 9 (IC50s = >20,408, >40,000, and >15,000 nM, respectively), as well as 20 additional methyltransferases and a panel of ion channels, receptors, and transporters at 10 μM. GSK3368715 (5 μM) inhibits the growth of patient-derived diffuse large B cell lymphoma (DLBCL) cells. In vivo, GSK3368715 (9.375-150 mg/kg) reduces tumor volume in Toledo DLBCL and BxPC-3 pancreatic adenosarcoma mouse xenograft models. It also reduces tumor growth in ACHN renal carcinoma and MDA-MB-468 breast cancer mouse xenograft models and a pancreatic adenocarcinoma patient-derived xenograft (PDX) mouse model when administered at doses of 150 and 300 mg/kg, respectively. | | References | 1.Fedoriw, A., Rajapurkar, S.R., O’Brien, S., et al.Anti-tumor activity of the type I PRMT inhibitor, GSK3368715, synergizes with PRMT5 inhibition through MTAP lossCancer Cell36(1)100-114.e125(2019) |
| | 1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-, hydrochloride (1:1) Preparation Products And Raw materials |
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