basic imformation2
| Price | USD1.00 |
| Packge | 1g |
- Min. Order:1g
- Supply Ability:500ton
- Time:2022-02-25
Product Details
- Product NameCediranib
- CAS No.288383-20-0
- EINECS No.670-946-2
- MFC25H27FN4O3
- MW450.51
- AppearanceSolidWhite to Off-White
- density 1.285
- Boiling point 626.6±55.0 °C(Predicted)
- storage temp. Sealed in dry,Store in freezer, under -20°C
- Melting point 135-138°C
| 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 | |
| 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]]. |
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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.
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Company Profile Introduction
- Since:2014-04-18
- Address: 2-1007, building 018, jinyuan business plaza, 152 huai andong road, yuhua district, shijiazhuang cit