| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| Other Sizes |
|
Purity: =99.93%
Axitinib (formerly AG013736; brand name Inlyta), is a potent, orally bioavailable, small molecule that inhibits multiple kinases and has the potential to treat cancer. In porcine aorta endothelial cells, it inhibits several kinases, including PDGFRβ, VEGFR1, VEGFR2, VEGFR3, and c-Kit, with IC50 values of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM, and 1.7 nM, respectively. Axitinib has an anti-angiogenic effect by inhibiting the proangiogenic cytokines PDGF and VEGF. On January 27, 2012, the FDA approved it as a treatment for renal cell carcinoma.
| Targets |
VEGFR1/FLT1 (IC50 = 0.1 nM); VEGFR2/Flk1 (IC50 = 0.18 nM); VEGFR2/KDR (IC50 = 0.2 nM); VEGFR3 (IC50 = 0.1 nM-0.3 nM nM); PDGFRβ (IC50 = 1.6 nM)
|
|---|---|
| ln Vitro |
Axitinib may inhibit VEGF-mediated endothelial cell viability, tube formation, and downstream signaling in addition to cellular autophosphorylation of VEGFR. Variable cell lines with IC50 values of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y), and 573 nM (non-VEGF stimulated HUVEC) are all inhibited by axitinib.[2]
|
| ln Vivo |
Axitinib shows primary inhibition against orthotopically transplanted models of colon cancer (HCT-116), melanoma (M24met), and renal cell carcinoma (SN12C).[1] In IGR-N91 fenografts, axitinib reduces the Mean Vessels Density (MVD) to 21 from 49 in controls and delays the tumor growth by 11.4 days when compared to the controls (p.o. 30 mg/kg).[2] In the BT474 breast cancer model, axitinib at doses of 10-100 mg/kg dramatically suppresses growth and alters the tumor microvasculature.[3] In a variety of tumor types, such as melanoma, thyroid cancer, non-small cell lung cancer, and renal cell carcinoma, axitinib has demonstrated single-agent activity.
|
| Enzyme Assay |
Generated are porcine aorta endothelial (PAE) cells that overexpress full-length VEGFR2, PDGFRβ, Kit, and NIH-3T3 cells that overexpress murine VEGFR2 (Flk-1) or PDGFRα. To prepare ELISA capture plates, 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 are coated on the 96-well plates. Next, an ELISA is used to measure RTK phosphorylation.
|
| Cell Assay |
A 96-well plate is seeded with 5 × 104 cells, and the cells are cultured for a full day. Concentrations of axitinib ranging from 1 nM to 10 μM are added to the cells. MTS tetrazolium substrate is used to measure cell viability after 72 hours, and IC50 values are computed.
|
| Animal Protocol |
Mice and Rats: Mice bearing 400–600 mm3 M24met xenograft tumors receive either a single Axitinib dose or 0.5% carboxymethylcellulose/H2O as a control. Samples of blood and tumor tissue are obtained for VEGFR-2 and pharmacokinetic analyses. The Bradford colorimetric assay is used to measure the total protein concentrations in tumor tissues.
Axitinib (30 mg/kg) is injected intraperitoneally twice into six-day-old Sprague-Dawley rats. Retinal tissue is extracted and lysed, animals are sacrificed, and immunoprecipitation and immunoblotting experiments are carried out. The Alpha Imager 8800 is used for densitometry analysis, and ECL-Plus is used for detection. |
| References |
| Molecular Formula |
C22H18N4OS
|
|---|---|
| Molecular Weight |
386.47
|
| Exact Mass |
386.12
|
| Elemental Analysis |
C, 68.37; H, 4.69; N, 14.50; O, 4.14; S, 8.30
|
| CAS # |
319460-85-0
|
| Related CAS # |
Axitinib-13C,d3;1261432-00-1;Axitinib-d3;1126623-89-9
|
| Appearance |
white to off-white solid powder
|
| SMILES |
CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)/C=C/C4=CC=CC=N4
|
| InChi Key |
RITAVMQDGBJQJZ-FMIVXFBMSA-N
|
| InChi Code |
InChI=1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+
|
| Chemical Name |
N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide
|
| Synonyms |
AG 013736; AG013736; Axitinib; AG 013736; Brand name: Inlyta
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5875 mL | 12.9376 mL | 25.8752 mL | |
| 5 mM | 0.5175 mL | 2.5875 mL | 5.1750 mL | |
| 10 mM | 0.2588 mL | 1.2938 mL | 2.5875 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05904730 | Active Recruiting |
Drug: tislelizumab combined with axitinib |
Neoadjuvant Therapy | Hongqian Guo | December 9, 2021 | Phase 2 |
| NCT03839498 | Recruiting | Drug: Axitinib | Pheochromocytoma Paraganglioma |
Columbia University | January 22, 2019 | Phase 2 |
| NCT05969496 | Recruiting | Drug: Axitinib Drug: Pembrolizumab |
Renal Cancer Kidney Cancer |
University of Colorado, Denver | October 14, 2023 | Phase 2 |
| NCT05817903 | Recruiting | Drug: Axitinib Drug: Nivolumab |
Metastatic Renal Cell Carcinoma |
Consorzio Oncotech | April 18, 2023 | Phase 2 |
| NCT04010071 | Recruiting | Drug: axitinib plus toripalimab | Hepatobiliary Neoplasm Liver Neoplasm |
Peking Union Medical College Hospital |
May 1, 2020 | Phase 2 |
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
