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Axitinib

Manufactured by Pfizer
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Axitinib is a laboratory equipment product manufactured by Pfizer. It is a tyrosine kinase inhibitor that targets the vascular endothelial growth factor (VEGF) receptors. Axitinib is designed for use in research and development applications.

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Lab products found in correlation

Crizotinib, by Pfizer (2 mentions) Anti chk1, by Cell Signaling Technology (1 mentions) Horseradish peroxidase hrp conjugated anti mouse igg, by Cell Signaling Technology (1 mentions) 5 dodecanoylaminofluorescein di β d galactopyranoside c12fdg, by Thermo Fisher Scientific (1 mentions) 10 n nonyl acridine orange, by Merck Group (1 mentions) 5 5 6 6 tetrachloro 1 1 3 3 tetraethylbenzimidazolylcarbocyanine iodide jc 1, by Thermo Fisher Scientific (1 mentions) 3 4 5 dimethylthiazol 2 yl 2 5 diphenyltetrazolium bromide mtt, by Merck Group (1 mentions) Hrp conjugated anti rabbit igg, by Cell Signaling Technology (1 mentions) Hoechst 33258, by Merck Group (1 mentions) Axitinib, by BioXCell (1 mentions) Anti mouse pd 1 antibody, by BioXCell (1 mentions) Anti mouse pd l1 antibody, by BioXCell (1 mentions) Cell counting kit 8 (cck8), by Dojindo Laboratories (1 mentions) Human recombinant fgf2, by Thermo Fisher Scientific (1 mentions) Neurocult chemical dissociation kit, by STEMCELL (1 mentions) Recombinant human egf, by R&D Systems (1 mentions) Human umbilical vein endothelial cells huvecs, by Lonza (1 mentions) U87 glioma cells, by American Type Culture Collection (1 mentions) Dulbecco modified eagle medium (dmem), by Thermo Fisher Scientific (1 mentions) Fetal bovine serum (fbs), by Thermo Fisher Scientific (1 mentions)

12 protocols using axitinib

1

Axitinib Modulates Neuropathic Pain

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Ten-week-old female Sprague Dawley rats were divided into three groups: sham (n = 5), HCl group (n = 5), and axitinib group (n = 5). One week after instillation (day 0), the axitinib group received oral administration of axitinib (Pfizer, 1 mg/kg) for 5 days (day 1–day 5), with a 2-day rest period. During axitinib administration, the manual von Frey test (Touch Test™ Sensory Evaluators; 58,011, Stoelting, IL, USA) was performed daily for pain evaluation. The initial stimulus was a 10 g (diameter: 5.07) filament. If there was no response, the next higher force filament was tested; if there was a response, the next filament with a lower force was tested. The test was continued until at least four records were obtained after the first change of response direction (positive to negative response or negative to positive response).
Shin J.H., Ryu C.M., Yu H.Y., Park Y.S., Shin D.M, & Choo M.S. (2023). Therapeutic effects of axitinib, an anti-angiogenic tyrosine kinase inhibitor, on interstitial cystitis. Scientific Reports, 13, 8329.
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2

Axitinib and Bortezomib Cytotoxicity Assay

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Axitinib (Inlyta®) was kindly provided by Pfizer (New York, NY). Bortezomib (BORT) was provided by Janssen-Cilag International N.V. (Beerse, Belgium). Mouse monoclonal anti-glyceraldehyde-3-phosphate dehydrogenase (GAPDH) Ab was from Origene (Rockville, MD). Mouse anti-p21 antibody (Ab) was purchased from Santa Cruz Biotechnology (Santa Cruz, CA). Rabbit anti-phospho-histone H2AX (Ser139), anti-Chk1-Ser345, anti-Chk1 and anti-caspase-3 Abs were purchased from Cell Signaling Technology (Danvers, MA). The following secondary antibodies were used: horseradish peroxidase (HRP)-conjugated anti-mouse IgG and HRP-conjugated anti-rabbit IgG (Cell Signaling Technology). Annexin V-fluorescein isothiocyanate (Annexin V-FITC) was purchased from eBioscience (Hatfield, UK). 5-dodecanoylaminofluorescein di-β-D- galactopyranoside (C12FDG) were from Invitrogen (San Diego, CA, USA). Bafilomycin A1, dimethyl sulfoxide (DMSO, used as vehicle), Hoechst 33258, propidium iodide (PI), ribonuclease A, 5-bromo-4-chloro-3-indolyl β-D- galactopyranoside (X-Gal), N-acetyl-L-cysteine (NAC), 10-N-nonyl acridine orange (NAO) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) were from Sigma Aldrich (St. Louis, MO). 5,5,6,6-tetrachloro-1,1,3,3-tetraethyl benzimidazolylcarbocyanine iodide (JC-1) was from Invitrogen (Carlsbad, CA).
Morelli M.B., Amantini C., Nabissi M., Cardinali C., Santoni M., Bernardini G., Santoni A, & Santoni G. (2016). Axitinib induces senescence-associated cell death and necrosis in glioma cell lines: The proteasome inhibitor, bortezomib, potentiates axitinib-induced cytotoxicity in a p21(Waf/Cip1) dependent manner. Oncotarget, 8(2), 3380-3395.
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3

Oral Gavage of Axitinib Suspension

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Axitinib (AG-13736, form IV, Pfizer, Inc.) was provided as a powder and suspended in 0.5% sodium carboxy-methyl cellulose solution for administration by oral gavage.
Rao S.S., Thompson C., Cheng J., Haimovitz-Friedman A., Powell S.N., Fuks Z, & Kolesnick R.N. (2014). Axitinib sensitization of high Single Dose Radiotherapy. Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology, 111(1), 88-93.
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4

Evaluating TKI and ICI Effects on RenCa Cells

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In vitro growth inhibitory effects of TKI and/or ICI on RenCa cells were assessed using Cell Counting Kit-8 (Dojindo Laboratories, Kumamoto, Japan). Briefly, 5 × 103 cells were seeded in each well of 96-well plates and allowed to attach overnight. The wells were treated with vehicle, axitinib (Pfizer, Inc., New York, NY, USA), anti-mouse PD-1 antibody (Bio X Cell, Lebanon, NH, USA), anti-mouse PD-L1 antibody (Bio X Cell), axitinib plus anti-mouse PD-1 antibody, or axitinib plus anti-mouse PD-L1 antibody. After 72 h of incubation, the number of cells was counted. Each assay was performed in triplicate.
Watanabe H., Matsushita Y., Tamura K., Motoyama D., Sugiyama T., Otsuka A, & Miyake H. (2023). Assessments of therapeutic effects according to timings for combined therapy with axitinib and immune check point inhibitor in a mouse renal cell carcinoma model. Scientific Reports, 13, 11361.
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5

Glioma Cells and Glioblastoma Stem Cell Culture

Cited 2 times
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Human U87 glioma cells were obtained from American Type Culture Collection (ATCC, Manassas, VA) and grown in complete Dulbecco’s modified Eagle’s medium (DMEM) supplemented with 10 % fetal calf serum at 37 °C and 5 % CO2. Human GSCs MGG4, MGG8, MGG18, BT74 were isolated as previously described [28 (link),30 (link)], and maintained as spheres in serum-free medium containing 20 ng/mL recombinant human EGF (R&D systems) and 20 ng/mL recombinant human FGF2 (Peprotech). GSCs were passaged by dissociating neurospheres using the Neuro-Cult Chemical Dissociation Kit (StemCell Technologies). Mouse 005 GSCs were provided by Dr. I. Verma (Salk Institute for Biological Studies, La Jolla, CA) [33 (link), 34 (link)]. Human umbilical vein endothelial cells (HUVECs) were purchased from Lonza. Human brain microvascular endothelial cells (HBMECs) were obtained from Dr. Ken Arai (MGH). Axitinib (Pfizer Inc) was provided by Pfizer and dissolved in DMSO as a 25 mM stock solution for in vitro studies. The final concentrations added to cells had less than 0.5 % DMSO, which was nontoxic to cells.
Lu L., Saha D., Martuza R.L., Rabkin S.D, & Wakimoto H. (2014). Single agent efficacy of the VEGFR kinase inhibitor axitinib in preclinical models of glioblastoma. Journal of neuro-oncology, 121(1), 91-100.
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6

Rat 9L Gliosarcoma Cell Culture

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The rat 9L gliosarcoma cell line, authenticated by and obtained from the UCSF Neurosurgery Tissue Bank (San Francisco, CA), was grown at 37°C in a humidified, 5% CO2 atmosphere in 10% FBS, 100 units/ml penicillin, and 100 μg/ml streptomycin containing DMEM culture medium. CPA was purchased from Sigma Chemical Co. (St. Louis, MO), sorafenib was purchased from LC Labs (Woburn, MA), axitinib was a gift from Pfizer (New York, NY), and DC101 was a gift from ImClone Systems (New York, NY). Fetal bovine serum (FBS) and DMEM were purchased from Invitrogen (Frederick, MD).
Doloff J.C., Chen C.S, & Waxman D.J. (2014). Anti-tumor innate immunity activated by intermittent metronomic cyclophosphamide treatment of 9L brain tumor xenografts is preserved by anti-angiogenic drugs that spare VEGF receptor 2. Molecular Cancer, 13, 158.
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7

Pfizer's Anti-Cancer Compounds: Axitinib and Crizotinib

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The following compounds were generated at Pfizer: axitinib (AG013736; trade name Inlyta®) [23 (link)] and crizotinib (PF-02341066; trade name Xalkori®) [24 (link)].
Eswaraka J., Giddabasappa A., Han G., Lalwani K., Eisele K., Feng Z., Affolter T., Christensen J, & Li G. (2014). Axitinib and crizotinib combination therapy inhibits bone loss in a mouse model of castration resistant prostate cancer. BMC Cancer, 14, 742.
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8

Axitinib and Tislelizumab for Cancer

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The control group received axitinib (specification: 5 mg/tablet, batch number: 20191123, approval number: h20150221, Pfizer manufacturing Deutschland GmbH), orally twice a day. After two consecutive weeks of administration, it can be increased to 7 mg each time within the safety threshold. After another two consecutive weeks of administration, it can be further increased to a maximum of 10 mg each time, twice a day. In cases of adverse reactions, the dose shall be adjusted according to its severity. The study group was additionally given tislelizumab injection (specification: 10 ml/100 mg, batch no. 20200108, approval no. s20190045, Baiji Shenzhou (Shanghai) Biotechnology Co., Ltd.) 200 mg intravenously once every 3 weeks. The dose is adjusted depending on the hematological or nonhematological toxicity during the treatment, and the treatment would be discontinued until the tumor progression or withdrawal occurs due to the life-threatening toxic reactions.
Wang Z., Chen J., Li Q., Li N., Yu J, & Liu F. (2022). The Effects of Axitinib plus Tislelizumab in the Treatment of Advanced Renal Cell Carcinoma. Journal of Oncology, 2022, 2700166.
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9

Axitinib and Dalantercept Combination Therapy

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Patients received continuous oral dosing of axitinib (Pfizer, New York, NY) at a starting dose level of 5 mg BID and either 0·9 mg/kg dalantercept (Acceleron Pharma Inc., Cambridge, MA) or placebo by subcutaneous injection every three weeks. Patients who tolerated axitinib 5 mg BID well for at least four consecutive weeks were permitted to have their axitinib dose increased from 5 to 7 mg BID and, subsequently, from 7 to 10 mg BID using the same tolerability and blood pressure criteria as previously established for axitinib.16 (link) Treatment was continued while tolerated and until progression of disease as defined by RECIST v1·1 with imaging to assess treatment response and disease progression every six weeks. Subsequently, they were contacted approximately every three months (± two weeks) to document survival status.
Voss M.H., Bhatt R.S., Vogelzang N.J., Fishman M., Alter R.S., Rini B.I., Beck J.T., Joshi M., Hauke R., Atkins M.B., Burgess E., Logan T.F., Shaffer D., Parikh R., Moazzam N., Zhang X., Glasser C., Sherman M.L, & Plimack E.R. (2019). A phase 2, randomized trial evaluating the combination of dalantercept plus axitinib in advanced clear cell renal cell carcinoma. Cancer, 125(14), 2400-2408.
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10

Preclinical Evaluation of Targeted Therapies

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Cabozantinib was purchased from Selleck Chemicals (Houston, TX) and used without further purification. Axitinib and crizotinib were graciously provided by Pfizer, Inc. (New York, NY). Intact male CB17 SCID mice were acquired from Taconic Farms (Hudson, NY) at 3 to 6 weeks of age. 18F–sodium fluoride (18F-NaF) was purchased from the radiopharmacy at Memorial Sloan-Kettering Cancer Center (MSKCC). Radioactivity was measured for dose preparation using a Capintec CRC-15R Dose Calibrator (Capintec, Ramsey, NJ).
Doran M.G., Spratt D.E., Wongvipat J., Ulmert D., Carver B.S., Sawyers C.L, & Evans M.J. (2014). Cabozantinib Resolves Bone Scans in Tumor-Naïve Mice Harboring Skeletal Injuries. Molecular imaging, 13, 10.2310/7290.2014.00026.
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