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| | KRN 633 Basic information |
| Product Name: | KRN 633 | | Synonyms: | KRN 633;N-[2-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propylurea;1-(2-chloro-4-(6,7-diMethoxyquinazolin-4-yloxy)phenyl)-3-propylurea;N-[2-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propylurea KRN633;VEGFR Tyrosine Kinase Inhibitor III, KRN633;KRN 633;KRN-633;CS-463;KRN633; KRN-633; KRN 633 | | CAS: | 286370-15-8 | | MF: | C20H21ClN4O4 | | MW: | 416.86 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 286370-15-8.mol |  |
| | KRN 633 Chemical Properties |
| Melting point | 231-232°C | | Boiling point | 545.6±50.0 °C(Predicted) | | density | 1.321 | | storage temp. | -20°C | | solubility | DMSO: soluble3mg/mL, clear (warmed) | | pka | 13.08±0.70(Predicted) | | form | powder | | color | white to beige |
| Hazard Codes | Xn | | Risk Statements | 22 | | WGK Germany | 3 |
| | KRN 633 Usage And Synthesis |
| Uses | KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM and also inhibits PDGFRα/β with IC50 of 965 nM/9850 nM. | | Uses | KRN 633 is an ATP-competitive inhibitor of vascular endothlial growth factor receptor tyrosine kinase (VEGFR). KRN 633 also suppresses VEGF-dependent activation of MAPK and cell proliferation and demonstrates antitumor and antiangiogenic activity by inhibiting vessel formation and vascular permeability in human tumor xenograft models. | | Biological Activity | krn 633 is a selective inhibitor of vegfr-1, vegfr-2 and vegfr-3 with ic50 value of 170 nm, 160 nm and 125 nm [1].vascular endothelial growth factor receptor (vegfr) is a protein and plays an important role in tumor angiogenesis by cooperating with its ligand vegf [1].krn 633 is a potent vegfr inhibitor. when tested with huvecs, krn 633 inhibited the cell proliferation that mediated by vegf with the ic50 value of 14.9 nmol/l and suppressed the capillary tube formation by ~50% at the dose of 10 nmol/l [1].in mid-pregnant mice model, krn633 was used at the dose of 5 mg/kg once daily from embryonic day 13.5 until the day of delivery and the effect on vascular growth was slightly delayed on postnatal day 4 (p4) and on p8 it was observed that krn633 resulted in the decreased numbers of central arteries and veins and abnormal branching of the central arteries [2]. when tested with athymic mouse xenograft ht29 cells model, administration of krn633 inhibited tumor growth as ~90% from the initial tumor volume rangs from 500-667 mm3, while had less effect du145 xenograft mouse models by inhibiting tumor angiogenesis and vascular permeability [1]. | | Biochem/physiol Actions | KRN633 is a cell-permeable; reversible and ATP-competitive inhibitor of vascular endothelial growth factor receptor tyrosine kinase (VEGFR) with IC50 values of 170, 160, and 125 nM for VEGFR-1, -2, -3, respectively. Krn633 inhibits PDGFR-α and c-Kit only at higher concentrations (IC50 = 0.97 and 4.33 μM, respectively) and is inactive towards a panel of 17 other kinases (IC50 >/= 10 μM). | | target | VEGFR3 | | references | [1]. nakamura, k., et al., krn633: a selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase that suppresses tumor angiogenesis and growth. mol cancer ther, 2004. 3(12): p. 1639-49.
[2]. morita, a., et al., treatment of mid-pregnant mice with krn633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, induces abnormal retinal vascular patterning in their newborn pups. birth defects res b dev reprod toxicol, 2014. 101(4): p. 293-9. |
| | KRN 633 Preparation Products And Raw materials |
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