| Identification | Back Directory | [Name]
JNJ-10198409 | [CAS]
627518-40-5 | [Synonyms]
RWJ 540973
JNJ-10198409
JNJ-10198409, Free Base
JNJ-10198409
(JNJ10198409)
JNJ-10198409 >=98% (HPLC), solid
PDGFR Tyrosine Kinase Inhibitor IV
JNJ-10198409 (This product is only available in Japan.)
PDGFR Tyrosine Kinase Inhibitor IV - CAS 627518-40-5 - Calbiochem
N-(3-Fluorophenyl)-6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-amine
N-(3-fluorophenyl)-2,4-dihydro-6,7-dimethoxy-Indeno[1,2-c]pyrazol-3-amine
3-Fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine
Indeno[1,2-c]pyrazol-3-amine, N-(3-fluorophenyl)-1,4-dihydro-6,7-dimethoxy-
RWJ 540973, 3-Fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine, N-(3-fluorophenyl)-2,4-dihydro-6,7-dimethoxy-Indeno[1,2-c]pyrazol-3-amine | [Molecular Formula]
C18H16FN3O2 | [MDL Number]
MFCD11045292 | [MOL File]
627518-40-5.mol | [Molecular Weight]
325.34 |
| Chemical Properties | Back Directory | [Melting point ]
171-173.5 °C | [Boiling point ]
528.8±50.0 °C(Predicted) | [density ]
1.366±0.06 g/cm3(Predicted) | [storage temp. ]
−20°C | [solubility ]
DMSO: >10mg/mL | [form ]
solid | [pka]
14.01±0.20(Predicted) | [color ]
off-white | [InChI]
1S/C18H16FN3O2/c1-23-15-7-10-6-14-17(13(10)9-16(15)24-2)21-22-18(14)20-12-5-3-4-11(19)8-12/h3-5,7-9H,6H2,1-2H3,(H2,20,21,22) | [InChIKey]
ZDNURMVOKAERHZ-UHFFFAOYSA-N | [SMILES]
COc1cc2Cc3c(Nc4cccc(F)c4)n[nH]c3-c2cc1OC |
| Hazard Information | Back Directory | [Uses]
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM)[1][2]. | [Biological Activity]
jnj-10198409 is a small molecule inhibitor of platelet-derived growth factor (pdgf-bb) tyrosine kinase [1].platelet-derived growth factor (pdgf) is a ubiquitous mitogen involved in regulating cell growth and division, embryonic development, cell proliferation, cell migration, and angiogenesis. overexpression of pdgf has been associated with several diseases such as atherosclerosis, fibrotic disorders and malignancies. inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (pdgf-bb) receptor can have potent antiangiogenic and antiproliferative activity. recombinant pdgf is used in medicine to help heal chronic ulcers and in orthopedic surgery and periodontistry to treat bone loss [2].in human coronary artery smooth muscle cells, jnj-10198409 inhibited the activity of platelet-derived growth factor (pdgf-bb) tyrosine kinase with an ic50 value of 4.2 nm when tested. jnj-10198409 was a competitive antagonist of the atp binding and hydrolysis at pdgf-bb receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis [1]. | [IC 50]
PDGFRβ: 4.2 nM (IC50); PDGFRα: 45 nM (IC50) | [storage]
Store at -20°C | [References]
[1] ho c y, ludovici d w, maharoof u s m, et al. (6, 7-dimethoxy-2, 4-dihydroindeno [1, 2-c] pyrazol-3-yl) phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells[j]. journal of medicinal chemistry, 2005, 48(26): 8163-8173.
[2] raines e w, bowen-pope d f, ross r. platelet-derived growth factor[m]//peptide growth factors and their receptors i. springer berlin heidelberg, 1990: 173-262. |
|
| Company Name: |
ChemCell Biomedicine Co.,Ltd.
|
| Telephone: |
020-13556033878 2965585218 13556033878 |
| Website: |
https://www.chemicalbook.com/ShowSupplierProductsList15061/0_EN.htm |
| Company Name: |
Energy Chemical
|
| Telephone: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Wuhan Topule
|
| Telephone: |
+86-02787215551 19945035818 |
| Website: |
http://www.topule.com/ |
|