Axitinib
Based on 42 publication(s) in Google Scholar
Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 319460-85-0
- Formula: C22H18N4OS
- Molecular Weight:386.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Axitinib
More- Cancer Cell. 2025 Apr 14;43(4):740-756.e8. [Abstract]
- Cell Metab. 2021 Oct 5;33(10):2021-2039.e8. [Abstract]
- Cell Stem Cell. 2019 Sep 5;25(3):373-387.e9. [Abstract]
- Cell Death Differ. 2026 Mar 23. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Adv Sci (Weinh). 2023 Jun;10(17):e2205915. [Abstract]
- J Nanobiotechnology. 2025 Apr 29;23(1):325. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Cancer Lett. 2024 Nov 26:217339. [Abstract]
- Cell Death Dis. 2025 Feb 23;16(1):125. [Abstract]
- Adv Healthc Mater. 2025 Jan;14(2):e2401985. [Abstract]
- Int J Biol Macromol. 2024 Feb 5;262(Pt 1):129950. [Abstract]
- Acta Pharmacol Sin. 2025 Feb;46(2):292-307. [Abstract]
- Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
- Phytomedicine. 2025 Nov 25:148:157421. [Abstract]
- Sci Total Environ. 2023 Dec 10:903:166505. [Abstract]
- J Transl Med. 2023 Sep 11;21(1):614. [Abstract]
- Cell Death Discov. 2026 Mar 28. [Abstract]
- Cell Rep. 2016 May 10;15(6):1144-60. [Abstract]
- Oncoimmunology. 2026 Dec 31;15(1):2689769. [Abstract]
- Front Immunol. 2021 Apr 30:12:649591. [Abstract]
- Biol Direct. 2025 Apr 2;20(1):43. [Abstract]
- Int J Mol Sci. 2022 Sep 14;23(18):10677. [Abstract]
- Bioorg Chem. 2025 Apr 5:160:108424. [Abstract]
- Int Immunopharmacol. 2024 May 30:133:112145. [Abstract]
- BMC Biol. 2024 Oct 1;22(1):222. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Cancers (Basel). 2023 Nov 12;15(22):5375. [Abstract]
- Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]
- Neurochem Res. 2025 Nov 12;50(6):356. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Mol Carcinog. 2024 Nov;63(11):2218-2236. [Abstract]
- J Cell Biochem. 2020 Mar;121(3):2343-2353. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2021 Nov 3;16(11):e0259241. [Abstract]
- Sci Pharm. 2023 Feb;91(1), 12.
- Res Sq. 2026 Jun 13.
- bioRxiv. 2026 May 13:2026.05.12.724633. [Abstract]
- bioRxiv. 2024 Jul 1:2024.06.27.601041. [Abstract]
- Research Square Preprint. 2022 Feb.
- Patent. US20170349880A1.
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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WB
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Flow Cytometry
All VEGFR Isoforms
More
Biological Activity
|
VEGFR1 0.1 nM (IC50) |
VEGFR2 0.2 nM (IC50) |
VEGFR3 0.1 nM (IC50) |
PDGFRβ 1.6 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 518A2 | IC50 |
4.4 μM
Compound: Axitinib
|
Cytotoxicity against human 518A2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Cytotoxicity against human 518A2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
|
[PMID: 31958738] |
| A549 | IC50 |
>25 μM
Compound: Axitinib
|
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| A549 | IC50 |
22.4 μM
Compound: Axitinib
|
Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay
Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay
|
[PMID: 30108994] |
| A549 | IC50 |
4.88 μM
Compound: II
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 31445229] |
| BaF3 | GI50 |
0.002 μM
Compound: 6
|
Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.005 μM
Compound: 6
|
Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.007 μM
Compound: 6
|
Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.012 μM
Compound: 6
|
Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.013 μM
Compound: 6
|
Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.014 μM
Compound: 6
|
Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.105 μM
Compound: 6
|
Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.108 μM
Compound: 6
|
Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.11 μM
Compound: 8
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.12 μM
Compound: 8
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.129 μM
Compound: 6
|
Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.156 μM
Compound: 6
|
Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.2 μM
Compound: 8
|
Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.24 μM
Compound: 8
|
Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.35 μM
Compound: 8
|
Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.406 μM
Compound: 6
|
Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
0.83 μM
Compound: 8
|
Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.84 μM
Compound: 8
|
Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
1.01 μM
Compound: 8
|
Inhibition of BCR/ABL H396P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL H396P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
1.46 μM
Compound: 8
|
Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
1.64 μM
Compound: 6
|
Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay
Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
1.64 μM
Compound: 8
|
Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay
Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
1.72 μM
Compound: 6
|
Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
1.82 μM
Compound: 6
|
Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
1.91 μM
Compound: 8
|
Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
2.02 μM
Compound: 6
|
Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 31046271] |
| BaF3 | GI50 |
2.63 μM
Compound: 8
|
Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| CHO | GI50 |
>10 μM
Compound: 8
|
Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay
Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| EA.hy 926 | IC50 |
6.1 μM
Compound: Axitinib
|
Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
|
[PMID: 31958738] |
| HCC1954 | GI50 |
2.7 μM
Compound: 1
|
Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay
|
[PMID: 23829549] |
| HCT-116 | IC50 |
>25 μM
Compound: Axitinib
|
Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| HCT-116 | IC50 |
>25 μM
Compound: Axitinib
|
Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| HCT-116 | IC50 |
1.5 μM
Compound: Axitinib
|
Cytotoxicity against wild type human HCT-116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Cytotoxicity against wild type human HCT-116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
|
[PMID: 31958738] |
| HCT-116 | IC50 |
1.6 μM
Compound: Axitinib
|
Cytotoxicity against human HCT-116 p53 mutant cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Cytotoxicity against human HCT-116 p53 mutant cells assessed as inhibition of cell growth after 72 hrs by MTT assay
|
[PMID: 31958738] |
| HEK-293T | IC50 |
46.82 μM
Compound: II
|
Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 31445229] |
| HepG2 | IC50 |
38.7 μM
Compound: Axitinib
|
Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay
Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay
|
[PMID: 30108994] |
| HL-60 | GI50 |
6.78 μM
Compound: 8
|
Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| HT-29 | IC50 |
13.12 μM
Compound: II
|
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 31445229] |
| K562 | GI50 |
0.94 μM
Compound: 8
|
Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| KB-V1 | IC50 |
12.9 μM
Compound: Axitinib
|
Cytotoxicity against multidrug resistant human KB-V1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
Cytotoxicity against multidrug resistant human KB-V1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
|
[PMID: 31958738] |
| MCF7 | GI50 |
0.97 μM
Compound: 1
|
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay
|
[PMID: 23829549] |
| MCF7 | GI50 |
2.3 μM
Compound: 3
|
Cytotoxicity against human MCF7 cells after 5 days by SRB assay
Cytotoxicity against human MCF7 cells after 5 days by SRB assay
|
[PMID: 24867403] |
| MCF7 | IC50 |
>25 μM
Compound: Axitinib
|
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| MDA-MB-231 | GI50 |
11 μM
Compound: 3
|
Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay
Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay
|
[PMID: 24867403] |
| MDA-MB-231 | GI50 |
7.3 μM
Compound: 1
|
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay
|
[PMID: 23829549] |
| MDA-MB-468 | GI50 |
1.3 μM
Compound: 1
|
Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay
|
[PMID: 23829549] |
| MDA-MB-468 | GI50 |
2.8 μM
Compound: 3
|
Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay
Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay
|
[PMID: 24867403] |
| MEC1 | GI50 |
1.54 μM
Compound: 8
|
Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| MEG-01 | GI50 |
0.97 μM
Compound: 8
|
Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| NHDF | IC50 |
>25 μM
Compound: Axitinib
|
Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| OCI-AML2 | GI50 |
2.36 μM
Compound: 8
|
Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| PC-3 | IC50 |
16.43 μM
Compound: II
|
Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 31445229] |
| Sf9 | IC50 |
0.0002 μM
Compound: 8
|
Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
|
[PMID: 30317026] |
| Sf9 | IC50 |
0.001 μM
Compound: 8
|
Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8
Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8
|
[PMID: 30317026] |
| Sf9 | IC50 |
0.092 μM
Compound: 8
|
Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G
Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G
|
[PMID: 30317026] |
| Sf9 | IC50 |
0.17 μM
Compound: 8
|
Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
|
[PMID: 30317026] |
| Sf9 | IC50 |
39 nM
Compound: II
|
Inhibition of recombinant human N-terminal GST-tagged VEGFR2 (805 to 1356 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 45 mins by kinase-Glo luminescent assay
Inhibition of recombinant human N-terminal GST-tagged VEGFR2 (805 to 1356 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 45 mins by kinase-Glo luminescent assay
|
[PMID: 31445229] |
| SK-BR-3 | GI50 |
3.8 μM
Compound: 1
|
Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay
Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay
|
[PMID: 23829549] |
| SK-BR-3 | GI50 |
4.6 μM
Compound: 3
|
Cytotoxicity against human SKBR3 cells after 5 days by SRB assay
Cytotoxicity against human SKBR3 cells after 5 days by SRB assay
|
[PMID: 24867403] |
| U-87MG ATCC | IC50 |
21.7 μM
Compound: II
|
Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 31445229] |
| U-937 | GI50 |
1.98 μM
Compound: 8
|
Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
Axitinib (AG-013736) is a potent and selective inhibitor of VEGFR 1 to 3. In transfected or endogenous RTK-expressing cells, Axitinib potently blocks growth factor-stimulated phosphorylation of VEGFR-2 and VEGFR-3 with average IC50 values of 0.2 and 0.1 to 0.3 nM, respectively. Cellular activity against VEGFR-1 is 1.2 nM (measured in the presence of 2.3% bovine serum albumin), equivalent to an absolute IC50 of ~0.1 nM, based on protein binding of Axitinib. The potency against murine VEGFR-2 (Flk-1) in Flk-1-transfected NIH-3T3 cells is 0.18 nM, similar to that of its human homologue. Axitinib shows ~8- to 25-fold higher IC50 against the closely related type III and V family RTKs, including PDGFR-β (1.6 nM), KIT (1.7 nM), and PDGFR-α (5 nM); nanomolar concentrations of Axitinib blocks PDGF BB-mediated human glioma U87MG cell (PDGFR-β-positive) migration but not proliferation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 319460-85-0
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Appearance Solid
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Molecular Weight 386.47
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Formula C22H18N4OS
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Color White to light yellow
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SMILES
O=C(C1=C(SC2=CC3=C(C(/C=C/C4=CC=CC=N4)=NN3)C=C2)C=CC=C1)NC
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Synonyms
AG-013736
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (42)
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Journal Impact Factor
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Most Recent
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Cancer Cell
2025 Apr 14;43(4):740-756.e8. PMID: 40086436 -
Cell Metab
The thermogenic activity of adjacent adipocytes fuels the progression of ccRCC and compromises anti-tumor therapeutic efficacy. [Abstract]2021 Oct 5;33(10):2021-2039.e8. PMID: 34508696 -
Cell Stem Cell
Generation of Human PSC-Derived Kidney Organoids with Patterned Nephron Segments and a De Novo Vascular Network. [Abstract]2019 Sep 5;25(3):373-387.e9. PMID: 31303547 -
Cell Death Differ
2026 Mar 23. PMID: 41872532 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
BEST1 Positive Monocytes in Circulation: Visualize Intratumoral Crosstalk between Cancer Cells and Monocytes. [Abstract]2023 Jun;10(17):e2205915. PMID: 37088729 -
J Nanobiotechnology
Single BMSC-derived cartilage organoids for gradient heterogeneous osteochondral regeneration by leveraging native vascular microenvironment. [Abstract]2025 Apr 29;23(1):325. PMID: 40301867 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Cancer Lett
Chemoresistance-motility signature of molecular evolution to chemotherapy in non-muscle-invasive bladder cancer and its clinical implications. [Abstract]2024 Nov 26:217339. PMID: 39608442 -
Cell Death Dis
STX17-DT facilitates axitinib resistance in renal cell carcinoma by inhibiting mitochondrial ROS accumulation and ferroptosis. [Abstract]2025 Feb 23;16(1):125. PMID: 39988631 -
Adv Healthc Mater
Macrophage Membrane-Biomimetic Multi-Layered Nanoparticles Targeting Synovial Angiogenesis for Osteoarthritis Therapy. [Abstract]2025 Jan;14(2):e2401985. PMID: 39402771 -
Int J Biol Macromol
Downregulation of VEGFA accelerates AGEs-mediated nucleus pulposus degeneration through inhibiting protective mitophagy in high glucose environments. [Abstract]2024 Feb 5;262(Pt 1):129950. PMID: 38320636 -
Acta Pharmacol Sin
VEGFD/VEGFR3 signaling contributes to the dysfunction of the astrocyte IL-3/microglia IL-3Rα cross-talk and drives neuroinflammation in mouse ischemic stroke. [Abstract]2025 Feb;46(2):292-307. PMID: 39478160 -
Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
Phytomedicine
Membrane cholesterol-dependent dual VEGFR2/FGFR1 inhibition by ginsenoside Rg3 to overcome gefitinib resistance in NSCLC. [Abstract]2025 Nov 25:148:157421. PMID: 41192258 -
Sci Total Environ
Azithromycin induces neurotoxicity in zebrafish by interfering with the VEGF/Notch signaling pathway. [Abstract]2023 Dec 10:903:166505. PMID: 37625730 -
J Transl Med
Tamoxifen exerts anti-peritoneal fibrosis effects by inhibiting H19-activated VEGFA transcription. [Abstract]2023 Sep 11;21(1):614. PMID: 37697303 -
Cell Death Discov
CXCR4, CXCR7 and PBRM1 are responsible for everolimus and cabozantinib resistance in human renal cancer cells. [Abstract]2026 Mar 28. PMID: 41896541 -
Cell Rep
Metabolic Symbiosis Enables Adaptive Resistance to Anti-angiogenic Therapy that Is Dependent on mTOR Signaling. [Abstract]2016 May 10;15(6):1144-60. PMID: 27134166 -
Oncoimmunology
Sequential axitinib and survivin vaccination unlock curative PD-1 immunotherapy in renal carcinoma. [Abstract]2026 Dec 31;15(1):2689769. PMID: 42343214 -
Front Immunol
Anti-Angiogenic Efficacy of PSORI-CM02 and the Associated Mechanism in Psoriasis In Vitro and In Vivo. [Abstract]2021 Apr 30:12:649591. PMID: 33995368 -
Biol Direct
GAMT facilitates tumor progression via inhibiting p53 in clear cell renal cell carcinoma. [Abstract]2025 Apr 2;20(1):43. PMID: 40176130 -
Int J Mol Sci
Chidamide plus Tyrosine Kinase Inhibitor Remodel the Tumor Immune Microenvironment and Reduce Tumor Progression When Combined with Immune Checkpoint Inhibitor in Naïve and Anti-PD-1 Resistant CT26-Bearing Mice. [Abstract]2022 Sep 14;23(18):10677. PMID: 36142591 -
Bioorg Chem
2025 Apr 5:160:108424. PMID: 40209351 -
Int Immunopharmacol
Comprehensive quantifications of tumour microenvironment to predict the responsiveness to immunotherapy and prognosis for paediatric neuroblastomas. [Abstract]2024 May 30:133:112145. PMID: 38691920 -
BMC Biol
VEGF-dependent testicular vascularisation involves MEK1/2 signalling and the essential angiogenesis factors, SOX7 and SOX17. [Abstract]2024 Oct 1;22(1):222. PMID: 39354506 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Cancers (Basel)
2023 Nov 12;15(22):5375. PMID: 38001635 -
Ther Adv Med Oncol
Axitinib overcomes multiple imatinib resistant cKIT mutations including the gatekeeper mutation T670I in gastrointestinal stromal tumors. [Abstract]2019 May 17:11:1758835919849757. PMID: 31205508
Axitinib purchased from MedChemExpress. Usage Cited in: Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]
Crystal violet staining of colonies from the four human GIST cell lines treated for 15 days with the indicated doses of Axitinib, imatinib, sunitinib, and regorafenib was performed.
Axitinib purchased from MedChemExpress. Usage Cited in: Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]
The effects of Axitinib (0–3 μM; 1 h) on cellular signaling, cell cycle progression, and apoptosis in human gastrointestinal stromal tumor (GIST) cancer cell lines were examined. Immunoblotting analysis of indicated proteins in c-KIT mediated signaling pathways of GIST-T1 was performed.
Axitinib purchased from MedChemExpress. Usage Cited in: Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]
Cell cycle analysis of the effect of Axitinib (0.3–3 μM; 24–48 h) at different concentrations in human GIST cell lines was measured by flow cytometry. Imatinib and sunitinib were used as positive controls.
Axitinib purchased from MedChemExpress. Usage Cited in: Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]
Cell viability assessment of primary cells from three GIST patients, relative to DMSO-treated condition, after 6 days of treatment with Axitinib (0.1–3 μM) at different concentrations using the Cell Titer-Glo assay was performed.
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Neurochem Res
A Novel Mutation in Exon 10 of the NOTCH3 Gene in Human Cerebral Microvascular Endothelial Cells Induces CADASIL-Like Pathology and the Therapeutic Effect of Edaravone Dexborneol on Hereditary and Non-hereditary Cerebral Small Vessel Disease. [Abstract]2025 Nov 12;50(6):356. PMID: 41222721 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Mol Carcinog
Pyroptosis-related gene GSDMC indicates poor prognosis and promotes tumor progression by activating the AKT/mTOR pathway in lung squamous cell carcinoma. [Abstract]2024 Nov;63(11):2218-2236. PMID: 39136610 -
J Cell Biochem
Vascular endothelial growth factor enhances tendon-bone healing by activating Yes-associated protein for angiogenesis induction and rotator cuff reconstruction in rats. [Abstract]2020 Mar;121(3):2343-2353. PMID: 31633245 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
PLoS One
The glutaminase inhibitor telaglenastat enhances the antitumor activity of signal transduction inhibitors everolimus and cabozantinib in models of renal cell carcinoma. [Abstract]2021 Nov 3;16(11):e0259241. PMID: 34731180
Axitinib purchased from MedChemExpress. Usage Cited in: PLoS One. 2021 Nov 3;16(11):e0259241. [Abstract]
Tumor volumes were measured in mice implanted subcutaneously with Caki-1 RCC cells and treated with either vehicle, Axitinib (25 mg/kg dosed orally QD) alone, or combinations of telaglenastat with each.
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Axitinib purchased from MedChemExpress. Usage Cited in: Sci Pharm. 2023 Feb;91(1), 12.
Axitinib (1, 10, 30 µM; 24 h) inhibits viability of MCF-7 cells.
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bioRxiv
A TSST-1 structural motif disrupts endothelial programs required for vascular regeneration. [Abstract]2026 May 13:2026.05.12.724633. PMID: 42182398 -
bioRxiv
Sulfur Amino Acid Restriction Enhances Exercise Capacity in Mice by Boosting Fat Oxidation in Muscle. [Abstract]2024 Jul 1:2024.06.27.601041. PMID: 39005372 -
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Solvent & Solubility
DMSO : 20.83 mg/mL (53.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.38 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 20% HP-β-CD/10 mM Citrate pH 2.0
Solubility: 8.33 mg/mL (21.55 mM); Clear solution; Need ultrasonic and adjust pH to 3 with H2O
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Endothelial or tumor cells are starved for 18 h in the presence of either 1% FBS (HUVEC) or 0.1% FBS (tumor cells). Axitinib is added and cells are incubated for 45 min at 37°C in the presence of 1 mM Na3VO4. The appropriate growth factor is added to the cells, and after 5 min, cells are rinsed with cold PBS and lysed in the lysis buffer and a protease inhibitor cocktail. The lysates are incubated with immunoprecipitation antibodies for the intended proteins overnight at 4°C. Antibody complexes are conjugated to protein A beads and supernatants are separated by SDS-PAGE[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice and Rats[2]
Mice with M24met xenograft tumors (400-600 mm3) are administered with a single dose of Axitinib or the control (0.5% carboxymethylcellulose/H2O). Blood and tumor tissue samples are collected for pharmacokinetic and VEGFR-2 measurements. Total protein concentrations in tumor tissues are determined using the Bradford colorimetric assay.
Six-day-old Sprague-Dawley rats are given two i.p. injections of Axitinib (30 mg/kg ). Animals are sacrificed, retinas are collected and lysed, and immunoprecipitation/immunoblotting experiments are done. ECL-Plus is used for detection and densitometry analysis is done using the Alpha Imager 8800.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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Handling Instructions (2659 KB)
References
[1]. Fenton BM, et al. The addition of AG-013736 to rractionated radiation improves tumor response without functionally normalizing the tumor vasculature. Cancer Res. 2007 Oct 15;67(20):9921-8. [Content Brief]
[2]. Hu-Lowe DD, et al. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res. 2008 Nov 15;14(22):7272-83 [Content Brief]
[3]. Allen E, et al. Metabolic Symbiosis Enables Adaptive Resistance to Anti-angiogenic Therapy that Is Dependent on mTOR Signaling. Cell Rep. 2016 May 10;15(6):1144-60. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5875 mL | 12.9376 mL | 25.8752 mL | 64.6881 mL |
| 5 mM | 0.5175 mL | 2.5875 mL | 5.1750 mL | 12.9376 mL | |
| 10 mM | 0.2588 mL | 1.2938 mL | 2.5875 mL | 6.4688 mL | |
| 15 mM | 0.1725 mL | 0.8625 mL | 1.7250 mL | 4.3125 mL | |
| 20 mM | 0.1294 mL | 0.6469 mL | 1.2938 mL | 3.2344 mL | |
| 25 mM | 0.1035 mL | 0.5175 mL | 1.0350 mL | 2.5875 mL | |
| 30 mM | 0.0863 mL | 0.4313 mL | 0.8625 mL | 2.1563 mL | |
| 40 mM | 0.0647 mL | 0.3234 mL | 0.6469 mL | 1.6172 mL | |
| 50 mM | 0.0518 mL | 0.2588 mL | 0.5175 mL | 1.2938 mL |