Vatalanib - CAS 212141-54-3
Catalog number: B0084-341508
Category: Inhibitor
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Molecular Formula:
C20H15ClN4
Molecular Weight:
346.81
COA:
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Targets:
VEGFR
Description:
Vatalanib, also called as PTK 787 or CGP 797870, is a small molecule that interacts reversibly and competitively at the ATP-binding site of the receptor tyrosine kinase domain to inhibit autophosphorylation. It targets all known VEGFR tyrosine kinases.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-341508 100 mg $198 In stock
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Purity:
>98%
Related CAS:
212141-51-0; 212142-18-2
Appearance:
Solid Powder
Synonyms:
N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine; PTK787; PTK 787; PTK-787; ZK 222584; ZK222584; ZK-222584; CGP 79787; CGP-797870; ZK-232934; CGP79787D; ZK 222584; CGP-7978
Solubility:
Soluble in DMSO.
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -67℃ for long term (months to years).
MSDS:
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Shelf Life:
2 years
Boiling Point:
587.8ºC at 760 mmHg
Melting Point:
209-212ºC
Density:
1.33 g/cm3
InChIKey:
YCOYDOIWSSHVCK-UHFFFAOYSA-N
InChI:
InChI=1S/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)
Canonical SMILES:
C1=CC=C2C(=C1)C(=NN=C2NC3=CC=C(C=C3)Cl)CC4=CC=NC=C4
1.2D and 3D similarity landscape analysis identifies PARP as a novel off-target for the drug Vatalanib.
Gohlke BO1, Overkamp T2, Richter A3, Richter A4, Daniel PT5,6,7, Gillissen B8,9, Preissner R10,11. BMC Bioinformatics. 2015 Sep 24;16:308. doi: 10.1186/s12859-015-0730-x.
BACKGROUND: Searching for two-dimensional (2D) structural similarities is a useful tool to identify new active compounds in drug-discovery programs. However, as 2D similarity measures neglect important structural and functional features, similarity by 2D might be underestimated. In the present study, we used combined 2D and three-dimensional (3D) similarity comparisons to reveal possible new functions and/or side-effects of known bioactive compounds.
2.Vatalanib sensitizes ABCB1 and ABCG2-overexpressing multidrug resistant colon cancer cells to chemotherapy under hypoxia.
To KK1, Poon DC2, Wei Y3, Wang F4, Lin G5, Fu LW6. Biochem Pharmacol. 2015 Sep 1;97(1):27-37. doi: 10.1016/j.bcp.2015.06.034. Epub 2015 Jul 20.
Cancer microenvironment is characterized by significantly lower oxygen concentration. This hypoxic condition is known to reduce drug responsiveness to cancer chemotherapy via multiple mechanisms, among which the upregulation of the ATP-binding cassette (ABC) efflux transporters confers resistance to a wide variety of structurally unrelated anticancer drugs. Vatalanib (PTK787/ZK22584) is a multitargeted tyrosine kinase inhibitor for all isoforms of VEGFR, PDGFR and c-Kit, which exhibit potent anticancer activity in vitro and in vivo. We investigated the potentiation effect of vatalanib on the anticancer activity of conventional cytotoxic drugs in colon cancer cell lines under both normoxic and hypoxic conditions. Mechanistically, vatalanib was found to inhibit ABCG2 and ABCB1 efflux activity, presumably by acting as a competitive inhibitor and interfering with their ATPase activity. Under hypoxic growth condition, ABCG2 and ABCB1-overexpressing cells sorted out by FACS technique as side population (SP) were found to be significantly more responsive to SN-38 (ABCG2 and ABCB1 substrate anticancer drug) in the presence of vatalanib.
3.Data showing the circumvention of oxaliplatin resistance by vatalanib in colon cancer.
To KK1, Poon DC1, Wei Y1, Wang F2, Lin G3, Fu LW2. Data Brief. 2016 Mar 2;7:437-44. doi: 10.1016/j.dib.2016.02.064. eCollection 2016.
We have recently reported that vatalanib, an orally active small molecule multi-tyrosine kinase inhibitor (Hess-Stumpp et al., 2005 [1]), can sensitize multidrug resistant (MDR) colon cancer cells to chemotherapy under hypoxia by inhibiting two MDR transporters ABCB1 and ABCG2 (To et al., 2015 [2]). This data article describes the possible circumvention of resistance to specifically platinum (Pt)-based anticancer drugs by vatalanib via inhibition of two other efflux transporters ABCC2 and ATP7A. Data from the flow cytometric transporter efflux assay showed specific inhibition of ABCC2 activity by vatalanib in stable transfected cells and ABCC2-overexpressing oxaliplatin-resistant colon cancer cells HCT116/Oxa. We also performed the transporter ABCC2 ATPase assay and showed an increase in ATP hydrolysis by ABCC2 in the presence of vatalanib. ATP7A mRNA expression was also shown to be upregulated in HCT116/Oxa cells. Vatalanib was shown to suppress this upregulated ATP7A expression.
4.Combination of vatalanib and a 20-HETE synthesis inhibitor results in decreased tumor growth in an animal model of human glioma.
Shankar A1, Borin TF2, Iskander A1, Varma NR3, Achyut BR1, Jain M1, Mikkelsen T4, Guo AM5, Chwang WB3, Ewing JR6, Bagher-Ebadian H6, Arbab AS1. Onco Targets Ther. 2016 Mar 9;9:1205-19. doi: 10.2147/OTT.S93790. eCollection 2016.
BACKGROUND: Due to the hypervascular nature of glioblastoma (GBM), antiangiogenic treatments, such as vatalanib, have been added as an adjuvant to control angiogenesis and tumor growth. However, evidence of progressive tumor growth and resistance to antiangiogenic treatment has been observed. To counter the unwanted effect of vatalanib on GBM growth, we have added a new agent known as N-hydroxy-N'-(4-butyl-2 methylphenyl)formamidine (HET0016), which is a selective inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthesis. The aims of the studies were to determine 1) whether the addition of HET0016 can attenuate the unwanted effect of vatalanib on tumor growth and 2) whether the treatment schedule would have a crucial impact on controlling GBM.
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CAS 212141-54-3 Vatalanib

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