LKT Labs

Biochemicals for Life Science Research

Vatalanib Dihydrochloride

Product ID V0376
Cas No. 212141-51-0
Purity ≥98%
Product Unit SizeCostQuantityStock
1 mg $48.60 In stock
5 mg $81.00 In stock
10 mg $105.80 In stock
25 mg $162.00 In stock
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Description

Vatalanib is an inhibitor of VEGFR that is currently in clinical trials for the treatment of myelodysplastic syndrome, lymphomas, non-small cell lung cancers (NSCLCs), and other cancers. Vatalanib exhibits anti-angiogenic, anti-metastatic, anticancer chemotherapeutic, and analgesic activities. In animal models with mammary carcinoma allografts, vatalanib decreases tumor vascularization. In animal models of pancreatic carcinoma, vatalanib inhibits tumor growth and metastasis and decreases microvessel density. Additionally, vatalanib decreases chronic neuropathic pain in animal models of chronic constriction injury, as inhibition of VEGFR2 inhibits signaling through neuropathic pain-mediating P2X (2/3) receptors.

Product Info

Cas No.

212141-51-0
Purity

≥98%
Formula

C20H15ClN4 • 2HCl
Formula Wt.

419.73
IUPAC Name

N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine;dihydrochloride
Synonym

PTK-787 Dihydrochloride, PTK 787 Dihydrochloride, PTK787 Dihydrochloride, ZK-222584 Dihydrochloride, ZK 222584 Dihydrochloride, ZK222584 Dihydrochloride, CGP-797870 Dihydrochloride, ZK232934 Dihydrochloride
Melting Point

268-270°C
Appearance

Off-white to pinkish powder

Shipping and Storage

Store Temp

Ambient
Ship Temp

Ambient

Downloads

MSDS

V0376 MSDS PDF
Info Sheet

V0376 Info Sheet PDF

References

Gupta P, Mulkey F, Hasserjian RP, et al. A phase II study of the oral VEGF receptor tyrosine kinase inhibitor vatalanib (PTK787/ZK222584) in myelodysplastic syndrome: Cancer and Leukemia Group B study 10105 (Alliance). Invest New Drugs. 2013 Oct;31(5):1311-20. PMID: 23700288.

Liu S, Xu C, Li G, et al. Vatalanib decrease the positive interaction of VEGF receptor-2 and P2X2/3 receptor in chronic constriction injury rats. Neurochem Int. 2012 May;60(6):565-72. PMID: 22361062.

Gauler TC, Besse B, Mauguen A, et al. Phase II trial of PTK787/ZK 222584 (vatalanib) administered orally once-daily or in two divided daily doses as second-line monotherapy in relapsed or progressing patients with stage IIIB/IV non-small-cell lung cancer (NSCLC). Ann Oncol. 2012 Mar;23(3):678-87. PMID: 21617019.

Hlushchuk R, Riesterer O, Baum O, et al. Tumor recovery by angiogenic switch from sprouting to intussusceptive angiogenesis after treatment with PTK787/ZK222584 or ionizing radiation. Am J Pathol. 2008 Oct;173(4):1173-85. PMID: 18787105.

Solorzano CC, Baker CH, Bruns CJ, et al. Inhibition of growth and metastasis of human pancreatic cancer growing in nude mice by PTK 787/ZK222584, an inhibitor of the vascular endothelial growth factor receptor tyrosine kinases. Cancer Biother Radiopharm. 2001 Oct;16(5):359-70. PMID: 11776753.

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