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Vatalanib (PTK787) 2HCl

Tyrosine kinase receptor inhibitor CAS# 212141-51-0

Vatalanib (PTK787) 2HCl

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Chemical structure

Vatalanib (PTK787) 2HCl

3D structure

Chemical Properties of Vatalanib (PTK787) 2HCl

Cas No. 212141-51-0 SDF Download SDF
PubChem ID 22386467 Appearance Powder
Formula C20H17Cl3N4 M.Wt 419.73
Type of Compound N/A Storage Desiccate at -20°C
Synonyms PTK787 dihydrochloride; PTK/ZK dihydrochloride; CGP-79787D dihydrochloride; CGP-79787 dihydrochloride; ZK-222584 dihydrochloride
Solubility DMSO : ≥ 125 mg/mL (297.81 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine;dihydrochloride
SMILES C1=CC=C2C(=C1)C(=NN=C2NC3=CC=C(C=C3)Cl)CC4=CC=NC=C4.Cl.Cl
Standard InChIKey AZUQEHCMDUSRLH-UHFFFAOYSA-N
Standard InChI InChI=1S/C20H15ClN4.2ClH/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);2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Vatalanib (PTK787) 2HCl

DescriptionVatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.In Vitro:Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 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 IC50 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[1]. 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[2].In Vivo: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[1].

References:
[1]. Wood JM, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000, 60(8 [2]. Murakami M, et al. Tyrosine kinase inhibitor PTK/ZK enhances the antitumor effects of interferon-α/5-fluorouracil therapy for hepatocellular carcinoma cells. Ann Surg Oncol. 2011, 18(2), 589-596. [3]. Wan J, et al. Local recurrence of small cell lung cancer following radiofrequency ablation is induced by HIF-1α expression in the transition zone. Oncol Rep. 2016 Mar;35(3):1297-308.

Protocol

Kinase Assay [1]
Each GST-fused kinase is incubated under optimized buffer conditions. ATP in a total volume of 30 μL in the presence or absence of a test substance (Vatalanib) for 10 min at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA[1].

Cell Assay [1]
Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin. After 24 h, growth medium is replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50 ng/mL), bFGF (0.5 ng/mL), or FCS (5%), in the presence or absence of Vatalanib. As a control, wells without growth factor are also included. After 24 h of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3' 5,5'-tetramethylbenzidine substrate[1].

Animal Administration [1]
A porous Teflon chamber (volume, 0.5 mL) is filled with 0.8% w/v agar containing heparin (20 units/mL) with or without growth factor (3 μg/mL human VEGF, 2 μg/mL human PDGF) is implanted s.c. on the dorsal flank of C57/C6 mice. The mice are treated with Vatalanib (12.5, 25 or 50 mg/kg dihydrochloride p.o. once daily) or vehicle (water) starting 1 day before implantation of the chamber and continuing for 5 days after. At the end of treatment, the mice are killed, and the chambers are removed. The vascularized tissue growing around the chamber is carefully removed and weighed, and the blood content is assessed by measuring the hemoglobin content of the tissue[1].

References:
[1]. Wood JM, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000, 60(8 [2]. Murakami M, et al. Tyrosine kinase inhibitor PTK/ZK enhances the antitumor effects of interferon-α/5-fluorouracil therapy for hepatocellular carcinoma cells. Ann Surg Oncol. 2011, 18(2), 589-596. [3]. Wan J, et al. Local recurrence of small cell lung cancer following radiofrequency ablation is induced by HIF-1α expression in the transition zone. Oncol Rep. 2016 Mar;35(3):1297-308.

Vatalanib (PTK787) 2HCl Dilution Calculator

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Vatalanib (PTK787) 2HCl Molarity Calculator

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Preparing Stock Solutions of Vatalanib (PTK787) 2HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3825 mL 11.9124 mL 23.8248 mL 47.6497 mL 59.5621 mL
5 mM 0.4765 mL 2.3825 mL 4.765 mL 9.5299 mL 11.9124 mL
10 mM 0.2382 mL 1.1912 mL 2.3825 mL 4.765 mL 5.9562 mL
50 mM 0.0476 mL 0.2382 mL 0.4765 mL 0.953 mL 1.1912 mL
100 mM 0.0238 mL 0.1191 mL 0.2382 mL 0.4765 mL 0.5956 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Vatalanib (PTK787) 2HCl

Vatalanib, also known as PTK787, is a potent vascular endothelial growth factor (VEGF) receptor tyrosine kinases inhibitor that inhibits VEGF receptor/KDR, VEGF receptor/Flt-1 and VEGF receptor/Flk with the half maximal inhibition concentration IC50 values of 0.037 μM, 0.077 μM and 0.27 μM respectively [1].

Vatalanib also inhibits other tyrosine kinases belonging to the same family of tyrosine kinase receptors as the VEGF receptors, including the platelet-derived growth factor receptor β tyrosine kinase (PDGFR-β), c-Kit and c-Fms, to a lesser degree with IC50 values of 0.58 μM, 0.73 μM and 1.4 μM respectively [1].

Vatalanib has been found to be potentially therapeutic for the treatment of angiogenesis-related diseases including solid tumors [1].

References:
[1] Wood JM, Bold G, Buchdunger E, Cozens R, Ferrari S, Frei J, Hofmann F, Mestan J, Mett H, O'Reilly T, Persohn E, Rösel J, Schnell C, Stover D, Theuer A, Towbin H, Wenger F, Woods-Cook K, Menrad A, Siemeister G, Schirner M, Thierauch KH, Schneider MR, Drevs J, Martiny-Baron G, Totzke F. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000 Apr 15;60(8):2178-89.

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Description

Vatalanib dihydrochloride (PTK787 dihydrochloride) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.

Keywords:

Vatalanib (PTK787) 2HCl,212141-51-0,PTK787 dihydrochloride; PTK/ZK dihydrochloride; CGP-79787D dihydrochloride; CGP-79787 dihydrochloride; ZK-222584 dihydrochloride,Natural Products,VEGFR, buy Vatalanib (PTK787) 2HCl , Vatalanib (PTK787) 2HCl supplier , purchase Vatalanib (PTK787) 2HCl , Vatalanib (PTK787) 2HCl cost , Vatalanib (PTK787) 2HCl manufacturer , order Vatalanib (PTK787) 2HCl , high purity Vatalanib (PTK787) 2HCl

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