KRN-633
KRN 633
CAS: 286370-15-8
Molecular Formula: C20H21ClN4O4
KRN-633 - Names and Identifiers
| Name | KRN 633 |
| Synonyms | KRN633 CS-463 KRN 633 KRN-633 KRN 633 KRN-633 VEGFR Tyrosine Kinase Inhibitor III, KRN633 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 N-[2-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propylurea KRN633 |
| CAS | 286370-15-8 |
KRN-633 - Physico-chemical Properties
| Molecular Formula | C20H21ClN4O4 |
| Molar Mass | 416.86 |
| Density | 1.321 |
| Melting Point | 231-232°C |
| Boling Point | 545.6±50.0 °C(Predicted) |
| Solubility | DMSO: soluble3mg/mL, clear (warmed) |
| Appearance | powder |
| Color | white to beige |
| pKa | 13.08±0.70(Predicted) |
| Storage Condition | -20°C |
| In vitro study | KRN 633 is a novel quinazoline urea derivative with strong inhibitory VEGFR-1, VEGFR-2 and VEGFR-3,IC50 of 170 nM,160 nM and 125 nM, respectively, for example, PDGF receptor (PDGFR)-α and-β,c-Kit, breast tumor kinase, and endometrial endothelial cell Kinase tyrosine kinase inhibition effect is not obvious, IC50 is 965, respectively, 9,850, 4,330, 9,200, and 9,900 nM. KRN 633 acts on HUVECs and effectively inhibits VEGFR-2 phosphorylation induced by ligand VEGF, with an IC50 of 1.16 nM. KRN 633 acts on endothelial cells to inhibit VEGF-dependent, but not bFGF-dependent, MAP kinase phosphorylation, and acts on ERK1 and ERK2 with IC50 of 3.51 nM and 6.08 nM, respectively. KRN 633 inhibit the proliferation of HUVECs driven by VEGF, IC50 of 14.9 nM, 3 M KRN633 only slightly blocked FGF driven proliferation. KRN 633 inhibited hypoxia-induced HIF-1α transcriptional activation by inhibiting Akt and ERK phosphorylation signaling pathways in a concentration-dependent manner, with an IC50 of 3.79 μm. |
| In vivo study | Although KRN633 is not toxic to various cancer cells in vitro, KRN633 has strong anticancer activity in vivo because of its inhibitory effect on tumor angiogenesis and vascular permeability. KRN633 treated A549,LC-6-LCK,HT29,Ls174T,LNCap and Du145 cells at a dose of 100 mg/kg per day, significantly inhibited tumor growth, and treated HT29 tumors twice a day at a dose of 100 mg/kg, the tumor growth inhibition rate was ~ 90%. Oral administration of KRN 633 at a dose of 300 mg/kg to mice in the second trimester of pregnancy decreased the amount of blood supplied to fetal tissues due to decreased vascularization in the placenta and fetal organs, thus, increased risk of induction of intrauterine growth restriction (IUGR). |
KRN-633 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| WGK Germany | 3 |
KRN-633 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.399 ml | 11.994 ml | 23.988 ml |
| 5 mM | 0.48 ml | 2.399 ml | 4.798 ml |
| 10 mM | 0.24 ml | 1.199 ml | 2.399 ml |
| 5 mM | 0.048 ml | 0.24 ml | 0.48 ml |
Last Update：2024-01-02 23:10:35
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Product Name: KRN 633 Visit Supplier Webpage Request for quotation
CAS: 286370-15-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 286370-15-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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