Vatalanib succinate - CAS 212142-18-2
Catalog number: B0084-014541
Category: Inhibitor
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Molecular Weight:
Vatalanib succinate is a potent and orally bioactive VEGFR inhibitor (IC50 =37 and 77 nM for VEGFR-2 and -1, respectively) exhibiting potential antineoplastic activity. Vatalanib binds to the protein kinase domain of VEGFR, and inhibits proliferation, migration and survival of HUVECs in vitro. Vatalanib also inhibits PDGFR-β, c-Kit and c-Fms.
Brife Description:
VEGFR inhibitor
≥99% by HPLC
Related CAS:
212141-51-0 (hydrochloride); 212141-54-3 (free base)
N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine succinate; CGP 79787D; PTK 787; ZK 222584; CGP79787D; PTK787; ZK222584; CGP-79787D; PTK-787; ZK-222584
Canonical SMILES:
1.New Insight into the Anti-liver Fibrosis Effect of Multitargeted Tyrosine Kinase Inhibitors: From Molecular Target to Clinical Trials.
Qu K;Huang Z;Lin T;Liu S;Chang H;Yan Z;Zhang H;Liu C Front Pharmacol. 2016 Jan 18;6:300. doi: 10.3389/fphar.2015.00300. eCollection 2015.
Tyrosine kinases (TKs) is a family of tyrosine protein kinases with important functions in the regulation of a broad variety of physiological cell processes. Overactivity of TK disturbs cellular homeostasis and has been linked to the development of certain diseases, including various fibrotic diseases. In regard to liver fibrosis, several TKs, such as vascular endothelial growth factor receptor, platelet-derived growth factor receptor, fibroblast growth factor receptor, and epidermal growth factor receptor kinases, have been identified as central mediators in collagen production and potential targets for anti-liver fibrosis therapies. Given the essential role of TKs during liver fibrogenesis, multitargeted inhibitors of aberrant TK activity, including sorafenib, erlotinib, imatinib, sunitinib, nilotinib, brivanib and vatalanib, have been shown to have potential for treating liver fibrosis. Beneficial effects are observed by researchers of this field using these multitargeted TK inhibitors in preclinical animal models and in patients with liver fibrosis. The present review will briefly summarize the anti-liver fibrosis effects of multitargeted TK inhibitors and molecular mechanisms.
2.Phase 1 study of PTK787/ZK 222584, a small molecule tyrosine kinase receptor inhibitor, for the treatment of acute myeloid leukemia and myelodysplastic syndrome.
Roboz GJ;Giles FJ;List AF;Cortes JE;Carlin R;Kowalski M;Bilic S;Masson E;Rosamilia M;Schuster MW;Laurent D;Feldman EJ Leukemia. 2006 Jun;20(6):952-7.
PTK787/ZK 222584 (PTK/ZK) is an oral angiogenesis inhibitor targeting vascular endothelial growth factor (VEGF) receptor tyrosine kinases, including VEGFR-1/Flt-1, VEGFR-2/KDR, VEGFR-3/Flt-4, the platelet-derived growth factor receptor tyrosine kinase and the c-kit protein tyrosine kinase. The objective of this Phase I study was to evaluate the safety, tolerability, biologic activity and pharmacologic profile of PTK/ZK administered orally, twice daily, on a continuous dosing schedule in patients with primary refractory or relapsed acute myeloid leukemia (AML), secondary AML, poor-prognosis de novo AML or advanced myelodysplastic syndrome (MDS). Acute myeloid leukemia patients for whom PTK/ZK monotherapy was ineffective could receive PTK/ZK combined with standard induction chemotherapy. Sixty-three patients received PTK/ZK at doses of 500-1000 mg orally b.i.d. Safety and pharmacokinetic data were collected. Responses were evaluated according to standard bone marrow and peripheral blood criteria. At 1000 mg b.i.d., dose-limiting toxicities of lethargy, hypertension, nausea, emesis and anorexia were observed. Other adverse events related to PTK/ZK were dizziness, weakness, fatigue, diarrhea and pruritus; these were generally mild and reversible.
3.Small molecule tyrosine kinase inhibitors in the treatment of solid tumors: an update of recent developments.
Steeghs N;Nortier JW;Gelderblom H Ann Surg Oncol. 2007 Feb;14(2):942-53. Epub 2006 Nov 14.
Small molecule tyrosine kinase inhibitors (TKIs) are developed to block intracellular signaling pathways in tumor cells, leading to deregulation of key cell functions such as proliferation and differentiation. Over 25 years ago, tyrosine kinases were found to function as oncogenes in animal carcinogenesis; however, only recently TKIs were introduced as anti cancer drugs in human cancer treatment. Tyrosine kinase inhibitors have numerous good qualities. First, in many tumor types they tend to stabilize tumor progression and may create a chronic disease state which is no longer immediately life threatening. Second, side effects are minimal when compared to conventional chemotherapeutic agents. Third, synergistic effects are seen in vitro when TKIs are combined with radiotherapy and/or conventional chemotherapeutic agents. In this article, we will give an update of the tyrosine kinase inhibitors that are currently registered for use or in an advanced stage of development, and we will discuss the future role of TKIs in the treatment of solid tumors. The following TKIs are reviewed: Imatinib (Gleevec/Glivec), Gefitinib (Iressa), Erlotinib (OSI-774, Tarceva), Lapatinib (GW-572016, Tykerb), Canertinib (CI-1033), Sunitinib (SU 11248, Sutent), Zactima (ZD6474), Vatalanib (PTK787/ZK 222584), Sorafenib (Bay 43-9006, Nexavar), and Leflunomide (SU101, Arava).
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CAS 212142-18-2 Vatalanib succinate

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