Axitinib

Catalog No.S1005 Batch:S100516

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Technical Data

Formula

C22H18N4OS
Molecular Weight 386.47 CAS No. 319460-85-0
Solubility (25°C)* In vitro DMSO 41 mg/mL (106.08 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
Targets
VEGFR1/FLT1 [1]
(Porcine aorta endothelial cells)		 VEGFR2/Flk1 [1]
(Porcine aorta endothelial cells)		 VEGFR2/KDR [1]
(Porcine aorta endothelial cells)		 VEGFR3 [1]
(Porcine aorta endothelial cells)		 PDGFRβ [1]
(Porcine aorta endothelial cells)		 View More
0.1 nM 0.18 nM 0.2 nM 0.1 nM-0.3 nM 1.6 nM
In vitro Axitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC). [2]
In vivo Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). [1] Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. [2] Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. [3] Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.
Features Superior as second-line therapy relative to sorafenib (current standard-of-care).

Protocol (from reference)

Kinase Assay:

[1]
  • Cellular receptor kinase phosphorylation assay

    Porcine aorta endothelial (PAE) cells, which overexpress full-length VEGFR2, PDGFRβ, Kit, and NIH-3T3, which overexpress murine VEGFR2 (Flk-1) or PDGFRα, are generated. The 96-well plates are coated with 100 μL/well of 2.5 μg/mL anti-VEGFR2 antibody, 0.75 μg/mL anti-PDGFRβ antibody, 0.25 μg/mL anti-PDGFRα antibody, 0.5 μg/mL anti-KIT antibody, or 1.20 μg/mL anti-Flk-1 antibody to prepare ELISA capture plates. Then phosphorylation of RTK is measured by ELISA.
Cell Assay:

[2]
  • Cell lines

    HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cells

  • Concentrations

    1 nM - 10 μM

  • Incubation Time

    72 hours

  • Method

    Cells are seeded in a 96-well plate at a density of 5 × 104 and cultured for 24 hours. Axitinib is added to the cells at concentrations ranging from 1 nM to 10 μM. Cell viability is measured after 72 hours by MTS tetrazolium substrate and IC50 values are calculated.
Animal Study:

[3]
  • Animal Models

    BT474 breast cancer cells are implanted subcutaneously into Immune-deficient female mice (Nu/nu; age 8-12 weeks).

  • Dosages

    10, 30 or 100 mg/kg

  • Administration

    Oral daily

Customer Product Validation

Data from [J Biomol Screen, 2011, 16, 141-154]

, , Oncogene, 2017, 36(36):5098-5109

, , Dr. Cheri Pasch of UW Madison

Data from [Data independently produced by , , J Biomol Screen, 2011,16: 141-154]

Selleck's Axitinib has been cited by 191 publications

Piezo1 regulates meningeal lymphatic vessel drainage and alleviates excessive CSF accumulation [ Nat Neurosci, 2024, 10.1038/s41593-024-01604-8] PubMed: 38528202
Targeting PDGF signaling of cancer-associated fibroblasts blocks feedback activation of HIF-1α and tumor progression of clear cell ovarian cancer [ Cell Rep Med, 2024, S2666-3791(24)00201-5] PubMed: 38670097
FLT1 activation in cancer cells promotes PARP-inhibitor resistance in breast cancer [ EMBO Mol Med, 2024, 10.1038/s44321-024-00094-2] PubMed: 38956205
The molecular basis of Abelson kinase regulation by its αI-helix [ Elife, 2024, 12RP92324] PubMed: 38588001
ROCK and the actomyosin network control biomineral growth and morphology during sea urchin skeletogenesis [ Elife, 2024, 12RP89080] PubMed: 38573316
Transcription of microRNAs is regulated by developmental signaling pathways and transcription factors [ Front Cell Dev Biol, 2024, 12:1356589] PubMed: 38721525
Cardiomyocyte crosstalk with endothelium modulates cardiac structure, function, and ischemia-reperfusion injury susceptibility through erythropoietin [ Front Physiol, 2024, 15:1397049] PubMed: 39011088
Xuebijing improves intestinal microcirculation dysfunction in septic rats by regulating the VEGF-A/PI3K/Akt signaling pathway [ World J Emerg Med, 2024, 15(3):206-213] PubMed: 38855370
Expression and Transcriptional Targets of TGFβ-RII in Paracentrotus lividus Larval Skeletogenesis [ Genesis, 2024, 62(4):e23614] PubMed: 39139086
Hematopoietic-specific heterozygous loss of Dnmt3a exacerbates colitis-associated colon cancer [ J Exp Med, 2023, 220(11)e20230011] PubMed: 37615936

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SHIPPING AND STORAGE
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