| Density | 1.3±0.1 g/cm3 |
|---|
| Boiling point | 626.6±55.0 °C at 760 mmHg |
|---|
| Molecular formula | C25H27FNfourOthree |
|---|
| Molecular weight | 450.505 |
|---|
| Flash point | 332.7±31.5 °C |
|---|
| Accurate mass | 450.206726 |
|---|
| PSA | 72.50000 |
|---|
| LogP | 4.80 |
|---|
| vapour pressure | 0.0±1.8 mmHg at 25°C |
|---|
| Refractive index | 1.642 |
|---|
| describe | Cediran IB Malte (AZD-2171 Malte) is a highly selective VEGFR2 inhibitor with oral activity. Its IC50 values for Flt1, KDR, Flt4, PDGFRα, PDGFRβ and c-Kit are less than 1, less than 3, 5, 5, 36 and 2nM, respectively. |
|---|
| Related categories | Signal path%3E%3Eautophagy%3E%3Eautophagy Signal path%3E%3EProtein tyrosine kinase%3E%3EPDGFR Research field%3E%3ECancer |
|---|
| target spot | Flt-1:5 nM (IC50) KDR:1 nM (IC50) Flt-4:3 nM (IC50) PDGFRα:36 nM (IC50) PDGFRβ:5 nM (IC50) c-Kit:2 nM (IC50) |
|---|
| In vitro study | In human umbilical vein endothelial cells, cetinib inhibited VEGF-stimulated proliferation and KDR phosphorylation with IC50 values of 0.4 and 0.5 nM, respectively. In the co-culture model of fibroblasts/endothelial cells with sprouting blood vessels, cetinib also reduced the area, length and branches under sub-nanomolar concentration of blood vessels [1]. |
|---|
| In vivo study | Cediranib can eliminate experimental (VEGF-induced) angiogenesis and inhibit intraosseous ossification in ovary or cartilage in corpus luteum development. Physiological processes are highly dependent on neovascularization. The growth of human tumor xenografts (colon, lung, prostate, breast and ovary) established in athymic mice was inhibited by cetinib in a dose-dependent manner. Long-term administration of 1.5mg/kg/day produced statistically significant inhibition in all models. Histological analysis of Calu-6 lung tumor treated with Cediranib showed that the microvessel density decreased within 52 hours and gradually increased with the duration of treatment. These changes indicate the degeneration of blood vessels in tumors. |
|---|
| Kinase experiment | A series of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFR-α, PDGFR-β, CSF-1R, Flt-3, FGFR1, Src, Abl] were used to determine the inhibitory activity of cetinib. Epidermal growth factor receptor (EGFR), ErbB2, Aur-A and aur-b were detected by ELISA. |
|---|
| Cell experiment | PDGF-AA induces the proliferation of MG63 osteosarcoma cells, which selectively activates PDGFR-α homodimer signal transduction. Cells were cultured in DMEM without phenol red containing 1% FCS stripped from activated carbon, 2mM glutamine and 1% non-essential amino acids for 24 hours. PDGF-AA ligand (50ng/mL) was added to cetinib or carrier, and the plate was re-cultured for 72 hours. Cell proliferation was determined by bromodeoxyuridine [1]. |
|---|
| Animal experiment | Rats: Young female Alderley Park rats (6 weeks old, Wistar-derived, n = 5) were given orally once a day, and were treated with cidinib (1.25-5mg/kg/day) or vehicle for 28 days. Additional rats (5 rats in each group) were treated with cetinib (5mg/kg/day) or vehicle for 28 days, and maintained for another 28 days without treatment to check the effect of compound withdrawal. Histological paraffin sections of femoral and tibial joints and ovaries were stained with H&E. The morphological image analysis of femur and tibia section was carried out, and the growth plate regions from femur and tibia in each joint were combined to analyze the effect of compound treatment. The area of corpus luteum in H&E stained ovarian sections was similarly determined by morphometric analysis [1]. Mice: The mice (day 0) carrying the established Calu-6 human lung tumor xenograft (0.2±0.01cm 3) were selected and treated with cetinib (6mg/kg/day, po) or carrier for a long time. On days 1, 2, 7, 14 and 21, tumors (6-15 in each group) were collected 4 hours after the last dose of cetinib or vector. Then cd31 was detected in the section using chromophore endpoint or fluorescence immunostaining [1]]. |
|---|
Inquiry guide
1. Please send the quantity(Weight) to us, we will arrange our sales to provide the one-for-one service for you.
2.Then we will provide the professional quotation list for you, it will be including all the factors in whole business process(Quality, shipping, payment, files etc.).
3.If you have many products need inquiry, please send the list for us, the product clear information includes CAS + Name + quantity(Weight), we will provide the complete solution for you. We also provide the customization product.
We are the Qualified suppliers of 24 famous listed international companies, including Pharmaceutical R&D agencies, New material factories, Wholesale trader of chemical reagent etc.
Profile
Hebei Zhuangkai Biotechnology Co. Ltd , mainly produces pharmaceutical raw
materials, pharmaceutical intermediates and refined products.Seek
development by credit reputation.Our products have a low price
advantage in Europe, South America and so on.
Superiorit
1.we have over 10 years experiencein this aera
2.As first cooperation,when we got your payment,would arrange cargo for
you.If the cargo delay,we would return payment.If the cargo lose,we'll reschedule it
for you
3.The most important thing,Regular customer,sample could be supply for you by free!
4.we are attention to every customer's requirements and make a good relationship with them.
Our company also has the advantage of high quality in Africa.In the
past two years, our products has reached more than 30 countries in the
world, and Europe.South America.North America, southeast Asia, Africa,
etc.
We welcome friends all over the world the best quality and best price
mutual cooperation and common development!
China
