Vatalanib
Based on 15 publication(s) in Google Scholar
Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 212141-54-3
- Formula: C20H15ClN4
- Molecular Weight:346.81
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Vatalanib
More- Bioact Mater. 2022 Jan 2:15:131-144. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Pharm Anal. 2024 Jan;14(1):100-114. [Abstract]
- Br J Pharmacol. 2019 Sep;176(17):3143-3160. [Abstract]
- JCI Insight. 2024 May 22;9(10):e166402. [Abstract]
- Int J Mol Sci. 2024 Nov 15;25(22):12277. [Abstract]
- Oncol Rep. 2016 Mar;35(3):1297-308. [Abstract]
- J Microbiol Biotechnol. 2015 Aug;25(8):1227-33. [Abstract]
- Drug Metab Pharmacokinet. 2017 Jun;32(3):179-188. [Abstract]
- Mutat Res. 2025 Sep 24:831:111916. [Abstract]
- Ulm University. 2023 Mar 21.
- Oxid Med Cell Longev. 2022 Jul 18:2022:2232365. [Abstract]
- Evid Based Complement Alternat Med. 2021 Apr 26:2021:5543259. [Abstract]
- Patent. US20170349880A1.
- Kitasato University. 2017.
All VEGFR Isoforms
More
Biological Activity
|
VEGFR2 37 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
21.16 μM
Compound: 8; PTK787
|
Inhibition of human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
Inhibition of human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
|
[PMID: 26590508] |
| A549 | IC50 |
21.16 μM
Compound: PTK-787
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 20537434] |
| CHO | IC50 |
0.016 μM
Compound: A, PTK-787
|
Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA
Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA
|
[PMID: 19124243] |
| EA.hy 926 | IC50 |
19.98 μM
Compound: 1
|
Cytotoxicity against human EAhy926 cells assessed as reduction in cell viability after 72 hrs by presto-blue assay
Cytotoxicity against human EAhy926 cells assessed as reduction in cell viability after 72 hrs by presto-blue assay
|
[PMID: 30776229] |
| EA.hy 926 | IC50 |
22.32 μM
Compound: Vatalanib
|
Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 72 hrs by PrestoBlue reagent based assay
Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 72 hrs by PrestoBlue reagent based assay
|
[PMID: 34459195] |
| HEK293 | IC50 |
0.021 μM
Compound: A
|
Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
|
[PMID: 16460936] |
| HEK293 | IC50 |
0.021 μM
Compound: A, PTK-787
|
Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA
Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA
|
[PMID: 19124243] |
| HT-29 | IC50 |
22.11 μM
Compound: 8; PTK787
|
Inhibition of human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay
Inhibition of human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay
|
[PMID: 26590508] |
| HT-29 | IC50 |
22.11 μM
Compound: PTK-787
|
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
|
[PMID: 20537434] |
| HUVEC | IC50 |
33 nM
Compound: 1, PTK-787
|
Inhibition of VEGF-induced HUVEC proliferation treated 1 hr before VEGF challenge measured 3 days by WST-8 assay
Inhibition of VEGF-induced HUVEC proliferation treated 1 hr before VEGF challenge measured 3 days by WST-8 assay
|
[PMID: 21074435] |
| HUVEC | IC50 |
33 nM
Compound: 1, PTK-787
|
Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced proliferation after 3 days by WST-8 assay
Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced proliferation after 3 days by WST-8 assay
|
[PMID: 21247763] |
| MDA-MB-231 | IC50 |
57.72 μM
Compound: 8; PTK787
|
Inhibition of human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
Inhibition of human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
|
[PMID: 26590508] |
| MDA-MB-231 | IC50 |
57.72 μM
Compound: PTK-787
|
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
|
[PMID: 20537434] |
| PBMC | IC50 |
>1 μM
Compound: 17 (PTK-787)
|
In vitro inhibitory concentration on the production of pro-inflammatory cytokine IL-2 in PBMC (Peripheral blood mononuclear cells) determined by IL-2 PBMC assay
In vitro inhibitory concentration on the production of pro-inflammatory cytokine IL-2 in PBMC (Peripheral blood mononuclear cells) determined by IL-2 PBMC assay
|
[PMID: 16107139] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 212141-54-3
-
Appearance Solid
-
Molecular Weight 346.81
-
Formula C20H15ClN4
-
Color Light yellow to yellow
-
SMILES
ClC1=CC=C(C=C1)NC2=NN=C(CC3=CC=NC=C3)C4=C2C=CC=C4
-
Synonyms
PTK787; ZK-222584; CGP-79787
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (15)
-
Journal Impact Factor
-
Most Recent
-
Bioact Mater
2022 Jan 2:15:131-144. PMID: 35386336 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Pharm Anal
Distinct molecular targets of ProEGCG from EGCG and superior inhibition of angiogenesis signaling pathways for treatment of endometriosis. [Abstract]2024 Jan;14(1):100-114. PMID: 38352946 -
Br J Pharmacol
Tanshinol borneol ester, a novel synthetic small molecule angiogenesis stimulator inspired by botanical formulations for angina pectoris. [Abstract]2019 Sep;176(17):3143-3160. PMID: 31116880 -
JCI Insight
Blocking the angiopoietin-2-dependent integrin β-1 signaling axis abrogates small cell lung cancer invasion and metastasis. [Abstract]2024 May 22;9(10):e166402. PMID: 38775153 -
Int J Mol Sci
Targeting Myeloid Cells in Head and Neck Squamous Cell Carcinoma: A Kinase Inhibitor Library Screening Approach. [Abstract]2024 Nov 15;25(22):12277. PMID: 39596341 -
Oncol Rep
Local recurrence of small cell lung cancer following radiofrequency ablation is induced by HIF-1α expression in the transition zone. [Abstract]2016 Mar;35(3):1297-308. PMID: 26750332 -
J Microbiol Biotechnol
Soluble Expression and Purification of the Catalytic Domain of Human Vascular Endothelial Growth Factor Receptor 2 in Escherichia coli. [Abstract]2015 Aug;25(8):1227-33. PMID: 25907066 -
Drug Metab Pharmacokinet
Precise prediction of activators for the human constitutive androstane receptor using structure-based three-dimensional quantitative structure-activity relationship methods. [Abstract]2017 Jun;32(3):179-188. PMID: 28412023 -
Mutat Res
Deciphering the molecular mechanism of YY1/HIF1A modulating ovarian cancer angiogenesis based on single-cell transcriptomics technology. [Abstract]2025 Sep 24:831:111916. PMID: 41072350 -
-
Oxid Med Cell Longev
Tetramethylpyrazine Protects Endothelial Injury and Antithrombosis via Antioxidant and Antiapoptosis in HUVECs and Zebrafish. [Abstract]2022 Jul 18:2022:2232365. PMID: 35898617 -
Evid Based Complement Alternat Med
Inhibitory Effects of Euphorbia ebracteolata Hayata Extract ECB on Melanoma-Induced Hyperplasia of Blood Vessels in Zebrafish Embryos. [Abstract]2021 Apr 26:2021:5543259. PMID: 33995546 -
-
Solvent & Solubility
DMSO : 62.5 mg/mL (180.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
-
Handling Instructions (2659 KB)
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 [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8834 mL | 14.4171 mL | 28.8342 mL | 72.0856 mL |
| 5 mM | 0.5767 mL | 2.8834 mL | 5.7668 mL | 14.4171 mL | |
| 10 mM | 0.2883 mL | 1.4417 mL | 2.8834 mL | 7.2086 mL | |
| 15 mM | 0.1922 mL | 0.9611 mL | 1.9223 mL | 4.8057 mL | |
| 20 mM | 0.1442 mL | 0.7209 mL | 1.4417 mL | 3.6043 mL | |
| 25 mM | 0.1153 mL | 0.5767 mL | 1.1534 mL | 2.8834 mL | |
| 30 mM | 0.0961 mL | 0.4806 mL | 0.9611 mL | 2.4029 mL | |
| 40 mM | 0.0721 mL | 0.3604 mL | 0.7209 mL | 1.8021 mL | |
| 50 mM | 0.0577 mL | 0.2883 mL | 0.5767 mL | 1.4417 mL | |
| 60 mM | 0.0481 mL | 0.2403 mL | 0.4806 mL | 1.2014 mL | |
| 80 mM | 0.0360 mL | 0.1802 mL | 0.3604 mL | 0.9011 mL | |
| 100 mM | 0.0288 mL | 0.1442 mL | 0.2883 mL | 0.7209 mL |