Axitinib (AG 013736) - Moligand™, 10mM in DMSO , Vascular endothelial growth factor receptor inhibitor, CAS No.319460-85-0, Vascular endothelial growth factor receptor inhibitor

CAS: 319460-85-0 Cat. No.: A408268 Peso molecular: 386.47 Número EC: 638-771-6

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

N-methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Axitinib (AG 013736) is a multi-target inhibitor ofVEGFR1,VEGFR2,VEGFR3, PDGFRβ and c-Kit withIC50of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
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).

In vivo

Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). 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. Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.
Cell Data

cell lines：DLBCL cells, SUDHL-6 cells

Concentrations：1 nM - 10 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Sinónimos

N-methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Axitinib (AG 013736) 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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Vascular endothelial growth factor receptor inhibitor

Propiedades del producto

• ALogP: 4.2

Nombres e identificadores

• Isómeros SMILES: CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)/C=C/C4=CC=CC=N4
• WGK Alemania: 3
• Peso molecular: 386.47
• Reaxy-Rn: 14436737
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14436737&ln=

Objetivos asociados (humanos)

CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (1 Activities)

Discover Target: CSF1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 (2 Activities)

Discover Target: FLT4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PLK4 Tchem Serine/threonine-protein kinase PLK4 (5 Activities)

Discover Target: PLK4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha (1 Activities)

Discover Target: PDGFRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRB Tclin Platelet-derived growth factor receptor beta (1 Activities)

Discover Target: PDGFRB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCR Tclin Breakpoint cluster region protein (1 Activities)

Discover Target: BCR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKB Tchem Aurora kinase B (1 Activities)

Discover Target: AURKB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKC Tchem Aurora kinase C (1 Activities)

Discover Target: AURKC

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT1 Tclin Vascular endothelial growth factor receptor 1 (3 Activities)

Discover Target: FLT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 (9 Activities)

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 (10 Activities)

Discover Target: ABL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit (7 Activities)

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 50 mg/mL (199.77 mM); Water: Insoluble; Ethanol: Insoluble

Referencias

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2. Fangjun Chen, Wenda Chen, Zhenxin Wang, Yingfei Peng, Beili Wang, Baishen Pan, Wei Guo.  (2023)  Development and clinical application of a liquid chromatography-tandem mass spectrometry-based assay to quantify eight tyrosine kinase inhibitors in human plasma.  Journal of Mass Spectrometry and Advances in the Clinical Lab,      [PMID:37234251] [10.1016/j.jmsacl.2023.05.001]

3. Zhao-Yang Wang, Hai-Long Wu, Yue-Yue Chang, Tong Wang, Wei Chen, Gao-Yan Tong, Ru-Qin Yu.  (2021)  Simultaneous determination of nine tyrosine kinase inhibitors in three complex biological matrices by using high-performance liquid chromatography–diode array detection combined with a second-order calibration method.  JOURNAL OF SEPARATION SCIENCE,  44  (21): (3914-3923).  [PMID:34463059] [10.1002/jssc.202100293]

4. Yue-Yue Chang, Hai-Long Wu, Huan Fang, Tong Wang, Yang-Zi Ouyang, Xiao-Dong Sun, Gao-Yan Tong, Yu-Jie Ding, Ru-Qin Yu.  (2020)  Comparison of three chemometric methods for processing HPLC-DAD data with time shifts: Simultaneous determination of ten molecular targeted anti-tumor drugs in different biological samples.  TALANTA,      [PMID:33379025] [10.1016/j.talanta.2020.121798]

5. Weizhen Chen, Kui Xu, Bailong Tao, Liangliang Dai, Yonglin Yu, Caiyun Mu, Xinkun Shen, Yan Hu, Ye He, Kaiyong Cai.  (2018)  Multilayered coating of titanium implants promotes coupled osteogenesis and angiogenesis in vitro and in vivo.  Acta Biomaterialia,      [PMID:29702291] [10.1016/j.actbio.2018.04.043]

6. Jianshuo Su, Jie Xu, Shufan Liu, Laura Machin Galarza, Shuangfeng Li, Huaizhen Zhang, Zhuang Ding, Jun Han, Min Liu, Yanna Zhao.  (2025)  Comparative study of binary and ternary axitinib solid dispersions: in vitro physicochemical characterization and in vivo pharmacokinetics.  JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY,      [PMID:] [10.1016/j.jddst.2025.107014]

7. Jianshuo Su, Shufan Liu, Zhuang Ding, Cuiying Zhang, Sisi Liu, Huaizhen Zhang, Jun Han, Zhengping Wang, Min Liu, Yanna Zhao.  (2025)  Laser-Triggered Liposomal Nanoparticles Combining Antiangiogenic and Photodynamic Therapy for Ocular Neovascularization.  ACS Applied Materials & Interfaces,      [PMID:41243313] [10.1021/acsami.5c17055]

8. Meng Zhang, Yumei Wang, Jiayi Wang, Jiayi Zuo, Feng Jiang, Feng Cao.  (2025)  Non-invasive co-delivery of Axitinib and telmisartan via LDH-based nanocarriers for synergistic VEGF/Ang-2 inhibition in ocular neovascular diseases.  JOURNAL OF CONTROLLED RELEASE,      [PMID:41448439] [10.1016/j.jconrel.2025.114574]