GW-786034

• CAT Number: A000546
• CAS Number: 444731-52-6
• Molecular Formula: C₂₁H₂₃N₇O₂S
• Molecular Weight: 437.52
• Purity: ≥95%
• Target: FGFR
• Solubility: >11mg/mL in DMSO
• Storage: -20°C
• InChI: InChI=1S/C21H23N7O2S/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25)
• InChIKey: CUIHSIWYWATEQL-UHFFFAOYSA-N
• SMILES: CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N

Pazopanib is an approved drug, is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits vascular endothelial growth factor receptors (VEGFR)-1, -2 and -3, c-kit and platelet derived growth factor receptor (PDGF-R), which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Reference

1: Yoshihiro T, Tsuchihashi K, Nio K, Arita S, Nakano T, Yasumatsu R, Jiroumaru
R, Ariyama H, Kusaba H, Oda Y, Akashi K, Baba E. Lingual alveolar soft part
sarcoma responsive to pazopanib: A case report. Medicine (Baltimore). 2017
Nov;96(44):e8470. doi: 10.1097/MD.0000000000008470. PubMed PMID: 29095301.

2: Ellawatty WEA, Masuo Y, Fujita KI, Yamazaki E, Ishida H, Arakawa H, Nakamichi
N, Abdelwahed R, Sasaki Y, Kato Y. Organic cation transporter 1 is responsible
for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib. Drug Metab
Dispos. 2017 Oct 31. pii: dmd.117.076554. doi: 10.1124/dmd.117.076554. [Epub
ahead of print] PubMed PMID: 29089306.

3: Kobayashi H, Okuma T, Oka H, Hirai T, Ohki T, Ikegami M, Sawada R, Shinoda Y,
Akiyama T, Sato K, Abe S, Kawano H, Goto T, Tanaka S. Neutrophil-to-lymphocyte
ratio after pazopanib treatment predicts response in patients with advanced
soft-tissue sarcoma. Int J Clin Oncol. 2017 Oct 31. doi:
10.1007/s10147-017-1199-6. [Epub ahead of print] PubMed PMID: 29086877.

4: Hioki T, Takama H, Makita S, Chen KR, Watanabe D, Akiyama M. Leg ulcers
associated with cutaneous vascular degeneration in a patient receiving pazopanib
chemotherapy. Eur J Dermatol. 2017 Oct 1;27(5):546-547. doi:
10.1684/ejd.2017.3092. PubMed PMID: 29084643.

5: Vogelzang NJ, Pal SK, Ghate SR, Swallow E, Li N, Peeples M, Zichlin ML,
Meiselbach MK, Perez JR, Agarwal N. Clinical and Economic Outcomes in Elderly
Advanced Renal Cell Carcinoma Patients Starting Pazopanib or Sunitinib Treatment:
A Retrospective Medicare Claims Analysis. Adv Ther. 2017 Oct 26. doi:
10.1007/s12325-017-0628-2. [Epub ahead of print] PubMed PMID: 29076108.

6: Bukhari N, Winquist E. Secondary polycythemia due to pazopanib in patients
with metastatic renal cell carcinoma. Can Urol Assoc J. 2017 Nov 11. doi:
10.5489/cuaj.4519. [Epub ahead of print] PubMed PMID: 29072563.

7: Stewart GD, Leibovich BC, Negrier S, Figlin RA. Adjuvant Pazopanib Does Not
PROTECT Against Recurrence of High-Risk, Initially Localized Renal Cell Cancer
but Does Provide Novel Insights. J Clin Oncol. 2017 Oct 25:JCO2017754242. doi:
10.1200/JCO.2017.75.4242. [Epub ahead of print] PubMed PMID: 29068785.

8: Deguchi S, Mitsuya K, Nakasu Y, Hayashi N, Katagiri H, Murata H, Wasa J,
Takahashi M, Endo M. Posterior reversible encephalopathy syndrome (PRES) induced
by pazopanib, a multi-targeting tyrosine kinase inhibitor, in a patient with
soft-tissue sarcoma: case report and review of the literature. Invest New Drugs.
2017 Oct 25. doi: 10.1007/s10637-017-0521-5. [Epub ahead of print] PubMed PMID:
29067537.

9: Koutsoukos K, Bamias A, Tzannis K, Espinosa Montaño M, Bozionelou V,
Christodoulou C, Stefanou D, Kalofonos H, Duran I, Papazisis K. Real-world
experience of everolimus as second-line treatment in metastatic renal cell cancer
after failure of pazopanib. Onco Targets Ther. 2017 Oct 6;10:4885-4893. doi:
10.2147/OTT.S141260. eCollection 2017. PubMed PMID: 29062235; PubMed Central
PMCID: PMC5640393.

10: Chellappan DK, Chellian J, Ng ZY, Sim YJ, Theng CW, Ling J, Wong M, Foo JH,
Yang GJ, Hang LY, Nathan S, Singh Y, Gupta G. The role of pazopanib on tumour
angiogenesis and in the management of cancers: A review. Biomed Pharmacother.
2017 Oct 17;96:768-781. doi: 10.1016/j.biopha.2017.10.058. [Epub ahead of print]
Review. PubMed PMID: 29054093.