Pynasunate
Vatalanib base
CAS: 212141-54-3
Molecular Formula: C20H15ClN4
Pynasunate - Names and Identifiers
| Name | Vatalanib base |
| Synonyms | Pynasunate Vatalanib base PTK787 free base Vatalanib free base (PTK787 free base Vatalanib (PTK787) Dihydrochloride Base Pynasunate, ZK222584, CGP-79787, PTK 787 N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)- 1-Phthalazinamine 1-PhthalazinaMine, N-(4-chlorophenyl)-4-(4-pyridinylMethyl)- (4-Chloro-phenyl)-(4-pyridin-4-ylmethyl-phthalazin-1-yl)-amine |
| CAS | 212141-54-3 |
| InChI | InChI=1/C20H15ClN4/c21-15-5-7-16(8-6-15)23-20-18-4-2-1-3-17(18)19(24-25-20)13-14-9-11-22-12-10-14/h1-12H,13H2,(H,23,25) |
Pynasunate - Physico-chemical Properties
| Molecular Formula | C20H15ClN4 |
| Molar Mass | 346.81 |
| Density | 1.330±0.06 g/cm3(Predicted) |
| Melting Point | 209-212° |
| Boling Point | 587.8±50.0 °C(Predicted) |
| Flash Point | 309.3°C |
| Vapor Presure | 8.48E-14mmHg at 25°C |
| pKa | 5.46±0.10(Predicted) |
| Storage Condition | 2-8°C(protect from light) |
| Refractive Index | 1.711 |
| In vitro study | Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC 50 of 270 nM, 730 nM and 580 nM, respectively. Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC 50 of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2. |
| In vivo study | Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes. |
Pynasunate - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.883 ml | 14.417 ml | 28.834 ml |
| 5 mM | 0.577 ml | 2.883 ml | 5.767 ml |
| 10 mM | 0.288 ml | 1.442 ml | 2.883 ml |
| 5 mM | 0.058 ml | 0.288 ml | 0.577 ml |
Last Update：2024-01-02 23:10:35
Pynasunate - Reference Information
| overview | tyrosine kinase inhibitor vatalani (vatalanib,PTK -787,ZK-222584) can effectively inhibit vascular endothelial growth factor receptor (VEGFR) family members, platelet-derived growth factor receptor 13(PDGFR ~) and c-Kit receptor kinase, and oral bioavailability is good. As early as 35 years ago, Folkman proposed that angiogenesis plays an important role in tumor growth and metastasis. Bevacizumab, an approved treatment for metastatic colorectal cancer, is an angiogenesis inhibitor. Vatalani can reversibly and competitively inhibit various receptor tyrosine kinases at the ATP binding site. Compared with bevacizumab, it has many advantages: it has an inhibitory effect on more receptor tyrosine kinases, and is effective orally, which is convenient for patients to take for a long time; the molecular weight is smaller, so it is easier to penetrate tumor cells and the blood-cerebrospinal fluid barrier than bevacizumab; in addition, antibodies may cause unpredictable adverse immune reactions and lead to toxicity, but vatalani does not have this problem. |
| pharmacokinetics | in vivo pharmacokinetic studies with unlabeled vataranib (vataranib base) show that this product can be quickly absorbed by oral administration on an empty stomach (t = 1-2h), but high-fat foods will slow down its absorption and prolong t to 4h; the absolute bioavailability of a single dose of this product is 58%, the steady-state apparent distribution volume is 3.3L/kg, the steady-state t1/2 is 5-6h, and the protein binding rate is 98.8%. This product is mainly metabolized by cytochrome P450CYP3A4, and only a small part is metabolized by CYP2D6 and CYP1A2. The main metabolites in the body are pyridine Ⅳ-oxide (CGP-84368/zK -260120) and 4-methyl-methanol pyridine Ⅳ-oxide (NVP-AAW-378/ZK-261557). The original drug and its metabolites can be excreted quickly in the body, mainly through bile and feces. After 22 days, the average cumulative excretion in urine is 23%(13%-29%), and the stool is 60%(42%-74%). |
| biological activity | Vatalanib(PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with an IC50 value of 37nM. |
| target | VEGFR2 37 nM (IC 50 ) |
| in vitro research | Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC 50 of 270 nM, 730 nM and 580 nM, respectively. Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC 50 of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors. A special study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2. |
| in vivo study | Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-drive angiogenesis model after once-daily oral dosing (25-100 mg/kg). in the same dose range, vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes. |
Last Update：2024-04-09 01:59:59
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Product Name: PTK787; ZK-222584; CGP-79787 Visit Supplier Webpage Request for quotationCAS: 212141-54-3
Tel: 609-228-6898
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tech@medchemexpress.com
Mobile: 609-228-6898
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