KRN 633
- Product Name
- KRN 633
- CAS No.
- 286370-15-8
- Chemical Name
- KRN 633
- Synonyms
- CS-463;KRN 633;KRN 633;KRN-633;KRN 633 USP/EP/BP;KRN633; KRN-633; KRN 633;VEGFR Tyrosine Kinase Inhibitor III, KRN633;KRN 633 (This product is unavailable in the U.S.);1-(2-chloro-4-(6,7-diMethoxyquinazolin-4-yloxy)phenyl)-3-propylurea;N-[2-Chloro-4-(6,7-dimethoxyquinazolin-4-yloxy)phenyl]-N'-propylurea;N-[2-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propylurea
- CBNumber
- CB42561482
- Molecular Formula
- C20H21ClN4O4
- Formula Weight
- 416.86
- MOL File
- 286370-15-8.mol
KRN 633 Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML0957
- Product name
- KRN633
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $133
- Updated
- 2022/05/15
- Product number
- 14871
- Product name
- KRN 633
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $51
- Updated
- 2024/03/01
- Product number
- 14871
- Product name
- KRN 633
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $99
- Updated
- 2024/03/01
- Product number
- 14871
- Product name
- KRN 633
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $184
- Updated
- 2024/03/01
- Product number
- 14871
- Product name
- KRN 633
- Purity
- ≥95%
- Packaging
- 50mg
- Price
- $773
- Updated
- 2024/03/01
KRN 633 Chemical Properties,Usage,Production
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
Raw materials
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View Lastest Price from KRN 633 manufacturers
- Product
- KRN 633 286370-15-8
- Price
- US $1000.00-950.00/KG
- Min. Order
- 1G
- Purity
- 98%
- Supply Ability
- 100kg
- Release date
- 2018-08-04