Axitinib

Catalog No.S1005 Batch:S100517

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Technical Data

Formula

C22H18N4OS
Molecular Weight 386.47 CAS No. 319460-85-0
Solubility (25°C)* In vitro DMSO 26 mg/mL (67.27 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 40% PEG 300 5%Tween80 50%ddH2O
1.85mg/ml Taking the 1 mL working solution as an example, add 50 μL of 37 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.2mg/ml Taking the 1 mL working solution as an example, add 50 μL of 4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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 180 publications

Hematopoietic-specific heterozygous loss of Dnmt3a exacerbates colitis-associated colon cancer [ J Exp Med, 2023, 220(11)e20230011] PubMed: 37615936
Hematopoietic-specific heterozygous loss of Dnmt3a exacerbates colitis-associated colon cancer [ J Exp Med, 2023, 220(11)e20230011] PubMed: 37615936
Single-cell RNA sequencing identifies critical transcription factors of tumor cell invasion induced by hypoxia microenvironment in glioblastoma [ Theranostics, 2023, 13(11):3744-3760] PubMed: 37441593
SMARCB1 regulates the hypoxic stress response in sickle cell trait [ Proc Natl Acad Sci U S A, 2023, 120(21):e2209639120] PubMed: 37186844
Selective induction of human renal interstitial progenitor-like cell lineages from iPSCs reveals development of mesangial and EPO-producing cells [ Cell Rep, 2023, S2211-1247(23)01614-5] PubMed: 38237600
Microenvironmental control of hematopoietic stem cell fate via CXCL8 and protein kinase C [ Cell Rep, 2023, 42(5):112528] PubMed: 37209097
A subset of VEGFR-TKIs activates AMPK in LKB1-mutant lung cancer [ Cancer Sci, 2023, 114(4):1651-1662] PubMed: 36459496
Potential therapeutic target secretogranin II might cooperate with hypoxia-inducible factor 1α in sunitinib-resistant renal cell carcinoma [ Cancer Sci, 2023, 10.1111/cas.15914] PubMed: 37545017
Potential therapeutic target secretogranin II might cooperate with hypoxia-inducible factor 1α in sunitinib-resistant renal cell carcinoma [ Cancer Sci, 2023, 114(10):3946-3956] PubMed: 37545017
Sphingosine-1-phosphate derived from PRP-Exos promotes angiogenesis in diabetic wound healing via the S1PR1/AKT/FN1 signalling pathway [ Burns Trauma, 2023, 11:tkad003] PubMed: 37251708

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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