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Semaxinib

(Synonyms: SU5416)

79 Cited Publications

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Based on 79 publication(s) in Google Scholar

Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC₅₀ of 1.23 μM.

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Pureté: 99.92%
CAS No.: 204005-46-9
Formule: C₁₅H₁₄N₂O
Masse moléculaire:238.28

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Semaxinib Chemical Structure

CAS No.: 204005-46-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (79)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
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Activité biologique

Description

Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC₅₀ of 1.23 μM^[1].

IC₅₀ & Target^[1]

Flk-1

1.23 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform VEGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
3T3	IC₅₀	20.3 μM Compound: 5a	Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation	[PMID: 12646019]
A-431	GI₅₀	37 μM Compound: Semaxanib	Growth inhibition of human A431 cells after 72 hrs by trypan blue assay Growth inhibition of human A431 cells after 72 hrs by trypan blue assay	[PMID: 29547832]
A-431	GI₅₀	37 μM Compound: Semaxanib	Growth inhibition of human A431 cells incubated for 72 hrs by trypan blue assay Growth inhibition of human A431 cells incubated for 72 hrs by trypan blue assay	[PMID: 30996779]
A-431	IC₅₀	0.085 μM Compound: 9, SU-5416	Antiangiogenic activity against human A431 cells Antiangiogenic activity against human A431 cells	[PMID: 20403693]
A-431	IC₅₀	12.9 μM Compound: SU-5416	Inhibition of VEGFR2 expressed in human A431 cells Inhibition of VEGFR2 expressed in human A431 cells	[PMID: 20558072]
A-431	IC₅₀	19.2 μM Compound: 7, SU-5416	Cytotoxicity against human A431 cells overexpressing EGFR incubated for 12 hrs measured after 36 hrs by CYQUANT assay Cytotoxicity against human A431 cells overexpressing EGFR incubated for 12 hrs measured after 36 hrs by CYQUANT assay	[PMID: 22370340]
A-431	IC₅₀	19.2 μM Compound: 9, SU-5416	Cytotoxicity against human A431 cells Cytotoxicity against human A431 cells	[PMID: 20403693]
A-431	IC₅₀	19.2 μM Compound: SU-5416, semaxanib	Cytotoxicity against human A431 cells Cytotoxicity against human A431 cells	[PMID: 18467105]
B16-F10	IC₅₀	0.0036 μM Compound: Semaxanib	Cytotoxicity against mouse B16F10 cells after 48 hrs by CCK8 assay Cytotoxicity against mouse B16F10 cells after 48 hrs by CCK8 assay	[PMID: 23777898]
BaF3	IC₅₀	>50 μM Compound: SU-5416	Growth inhibition of mouse BA/F3 cells assessed as incorporation of [3H]thymidine incorporation after 72 hrs by liquid scintillation counting Growth inhibition of mouse BA/F3 cells assessed as incorporation of [3H]thymidine incorporation after 72 hrs by liquid scintillation counting	[PMID: 20117004]
CHO	ED₅₀	930 nM Compound: SU-5416	Inhibition of VEGF-stimulated autophosphorylation of VEGF-receptor 2 (KDR) expressed in CHO cells Inhibition of VEGF-stimulated autophosphorylation of VEGF-receptor 2 (KDR) expressed in CHO cells	[PMID: 10882357]
CHO	IC₅₀	884 nM Compound: 3 (SU-5416)	Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells	[PMID: 12477352]
HeLa	GI₅₀	38 μM Compound: Semaxanib	Growth inhibition of human HeLa cells after 72 hrs by trypan blue assay Growth inhibition of human HeLa cells after 72 hrs by trypan blue assay	[PMID: 29547832]
HeLa	GI₅₀	38 μM Compound: Semaxanib	Growth inhibition of human HeLa cells incubated for 72 hrs by trypan blue assay Growth inhibition of human HeLa cells incubated for 72 hrs by trypan blue assay	[PMID: 30996779]
HeLa	IC₅₀	20 μM Compound: SU5416	Antiproliferative activity against human HeLa cells after 4 days by coulter counter method Antiproliferative activity against human HeLa cells after 4 days by coulter counter method	[PMID: 23124213]
HMEC-1	IC₅₀	15 μM Compound: SU5416	Antiproliferative activity against human HMEC1 cells after 7 days by coulter counter method Antiproliferative activity against human HMEC1 cells after 7 days by coulter counter method	[PMID: 23124213]
HUVEC	GI₅₀	13.6 μM Compound: Semaxanib	Growth inhibition of HUVEC incubated for 72 hrs by trypan blue assay Growth inhibition of HUVEC incubated for 72 hrs by trypan blue assay	[PMID: 30996779]
HUVEC	GI₅₀	13.6 μM Compound: SU5414, Semaxanib	Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability after 72 hrs by trypan blue assay Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability after 72 hrs by trypan blue assay	[PMID: 26318056]
HUVEC	IC₅₀	>50 μM Compound: 1	Evaluated for the inhibition of cell proliferation induced by EGF in HUVEC or NIH3T3 cells Evaluated for the inhibition of cell proliferation induced by EGF in HUVEC or NIH3T3 cells	[PMID: 10893303]
HUVEC	IC₅₀	0.04 μM Compound: 1	Evaluated for the inhibition of cell proliferation induced by VEGF in HUVEC or NIH3T3 cells Evaluated for the inhibition of cell proliferation induced by VEGF in HUVEC or NIH3T3 cells	[PMID: 10893303]
HUVEC	IC₅₀	4.54 μM Compound: 1	Evaluated for the inhibition of cell proliferation induced by PDGF in HUVEC or NIH3T3 cells Evaluated for the inhibition of cell proliferation induced by PDGF in HUVEC or NIH3T3 cells	[PMID: 10893303]
HUVEC	IC₅₀	50 μM Compound: 1	Evaluated for the inhibition of cell proliferation induced by FGF in HUVEC or NIH3T3 cells Evaluated for the inhibition of cell proliferation induced by FGF in HUVEC or NIH3T3 cells	[PMID: 10893303]
MCF7	IC₅₀	>50 μM Compound: SU-5416	Antiproliferative activity against estrogen-dependent breast cancer MCF7 cell line by MTS assay Antiproliferative activity against estrogen-dependent breast cancer MCF7 cell line by MTS assay	[PMID: 16213720]
MCF7	IC₅₀	0.0031 μM Compound: Semaxanib	Cytotoxicity against human MCF7 cells after 48 hrs by CCK8 assay Cytotoxicity against human MCF7 cells after 48 hrs by CCK8 assay	[PMID: 23777898]
MCF7	IC₅₀	1.9 μM Compound: SU5416	Antiproliferative activity against human MCF7 cells after 4 days by coulter counter method Antiproliferative activity against human MCF7 cells after 4 days by coulter counter method	[PMID: 23124213]
MDA-MB-231	IC₅₀	>50 μM Compound: SU-5416	Antiproliferative activity against estrogen-independent breast cancer MDA-MB-231 cell line by MTS assay Antiproliferative activity against estrogen-independent breast cancer MDA-MB-231 cell line by MTS assay	[PMID: 16213720]
MSTO-211H	GI₅₀	27 μM Compound: Semaxanib	Growth inhibition of human MSTO-211H cells after 72 hrs by trypan blue assay Growth inhibition of human MSTO-211H cells after 72 hrs by trypan blue assay	[PMID: 29547832]
MSTO-211H	GI₅₀	27 μM Compound: Semaxanib	Growth inhibition of human MSTO-211H cells incubated for 72 hrs by trypan blue assay Growth inhibition of human MSTO-211H cells incubated for 72 hrs by trypan blue assay	[PMID: 30996779]
NIH3T3	IC₅₀	1.04 μM Compound: 2	Inhibitory activity against Vascular endothelial growth factor receptor 2 (VEGF-R2) in NIH3T3 mouse fibroblast cells Inhibitory activity against Vascular endothelial growth factor receptor 2 (VEGF-R2) in NIH3T3 mouse fibroblast cells	[PMID: 10602697]
NIH3T3	IC₅₀	1.04 μM Compound: 5a	Inhibition of Vascular endothelial growth factor receptor in 3T3 cells Inhibition of Vascular endothelial growth factor receptor in 3T3 cells	[PMID: 12646019]
NIH3T3	IC₅₀	20.26 μM Compound: 2	Inhibitory activity against Platelet-derived growth factor receptor (PDGF-R) in NIH3T3 mouse fibroblast cells Inhibitory activity against Platelet-derived growth factor receptor (PDGF-R) in NIH3T3 mouse fibroblast cells	[PMID: 10602697]
NIH3T3	IC₅₀	4.05 μM Compound: 5a	Inhibition of PDGF-induced BrdU incorporation in 3T3 cells Inhibition of PDGF-induced BrdU incorporation in 3T3 cells	[PMID: 12646019]
PBMC	IC₅₀	0.005 μM Compound: 1 (SU-5416)	In vitro inhibitory concentration on the production of pro-inflammatory cytokine IL-2 in PBMC (Peripheral blood mononuclear cells) determined by IL-2 PBMC assay In vitro inhibitory concentration on the production of pro-inflammatory cytokine IL-2 in PBMC (Peripheral blood mononuclear cells) determined by IL-2 PBMC assay	[PMID: 16107139]
PC-3	IC₅₀	>50 μM Compound: SU-5416	Antiproliferative activity against androgen-independent prostate cancer PC3 cell line by MTS assay Antiproliferative activity against androgen-independent prostate cancer PC3 cell line by MTS assay	[PMID: 16213720]
SF-539	IC₅₀	2.4 μM Compound: SU-5416	Inhibition of PDGFRbeta in human SF539 cells by phosphotyrosine ELISA Inhibition of PDGFRbeta in human SF539 cells by phosphotyrosine ELISA	[PMID: 19748785]
Sf9	IC₅₀	0.17 μM Compound: SU-5416	Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells	[PMID: 20117004]
Sf9	IC₅₀	20.7 μM Compound: 23	Inhibition of human GST-fused ZAP-70 expressed in Sf9 cells Inhibition of human GST-fused ZAP-70 expressed in Sf9 cells	[PMID: 19674816]
Sf9	IC₅₀	3 μM Compound: SU5416	Inhibition of GST-Flt1 kinase domain (unknown origin) expressed in baculovirus infected Sf9 cells after 20 mins by scintillation counting Inhibition of GST-Flt1 kinase domain (unknown origin) expressed in baculovirus infected Sf9 cells after 20 mins by scintillation counting	[PMID: 23414235]
U-251	IC₅₀	12 μM Compound: 18, SU-5416	Inhibition of VEGFR2 tyrosine kinase activity in VEGF-stimulated human U251 cells after 60 mins by ELISA Inhibition of VEGFR2 tyrosine kinase activity in VEGF-stimulated human U251 cells after 60 mins by ELISA	[PMID: 22204741]
U-251	IC₅₀	12 μM Compound: 20	Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA	[PMID: 23434139]
U-251	IC₅₀	12 μM Compound: 27	Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis	[PMID: 23375090]
U-251	IC₅₀	12 μM Compound: 46, SU-5416	Inhibition of VEGFR2 phosphorylation in human U251 cells after 10 mins by FLISA Inhibition of VEGFR2 phosphorylation in human U251 cells after 10 mins by FLISA	[PMID: 20403700]
U-251	IC₅₀	12.9 nM Compound: Semaxanib	Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay	[PMID: 24890652]
U-251	IC₅₀	12.9 nM Compound: Semaxanib	Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method	[PMID: 25882519]
U-251	IC₅₀	12.9 nM Compound: semaxinib	Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA	[PMID: 24900865]
U-251	IC₅₀	12.9 μM Compound: SU-5416	Inhibition of VEGFR2 in human U251 cells by phosphotyrosine cell-based ELISA Inhibition of VEGFR2 in human U251 cells by phosphotyrosine cell-based ELISA	[PMID: 20092323]
U-251	IC₅₀	12.9 μM Compound: SU-5416	Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA	[PMID: 22739090]
U-251	IC₅₀	2.43 μM Compound: 7, SU-5416	Inhibition of VEGF-induced VEGFR2 autophosphorylation in human U251 cells incubated for 60 mins prior to VEGF-induction measured after 10 mins by phosphotyrosine ELISA Inhibition of VEGF-induced VEGFR2 autophosphorylation in human U251 cells incubated for 60 mins prior to VEGF-induction measured after 10 mins by phosphotyrosine ELISA	[PMID: 22370340]

In Vitro

Semaxinib (SU5416) inhibits VEGF-driven mitogenesis in a dose-dependent manner with an IC₅₀ of 0.04±0.02 μM (n=3). In contrast, Semaxinib (SU5416) blocks FGF-dependent mitogenesis of HUVECs with an IC₅₀ of 50 μM (n=10). An IC₅₀ of 20.26±5.2 μM, which is about 20-fold less in potency on PDGF-dependent autophosphorylation, is observed when SU5416 is tested in NIH 3T3 cells overexpressing the human PDGF receptor β^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Daily administration of Semaxinib (SU5416) (i.p., 3 mg/kg/day) inhibits the local growth of C6 tumors in the colon. A comparable level of growth inhibition (62% by day 16; P=0.001) is observed for tumors growing in the colon in comparison with ones growing in the hindflank region (54% by day 18; P=0.001). These results indicate that Semaxinib (SU5416) could inhibit tumor growth at a site other than the subcutaneous implantation site, where the preexisting vasculature may be different^[1]. Daily treatment with Semaxinib (SU5416) (25 mg/kg) results in a significantly lower tumor growth rate with tumor masses of up to 8% of that present in control animals by day 22 after implantation. Inhibition of tumor growth is clearly preceded by a marked reduction of the tissue area covered by the newly formed glioma microvasculature in the Semaxinib-treated group, indicating a reduced initial tumor vascularization^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 204005-46-9
Appearance Solid
Masse moléculaire 238.28
Formule C₁₅H₁₄N₂O
Color Brown to orange
SMILES

O=C(NC1=CC=CC=C/21)C2=C/C3=C(C)C=C(C)N3
Synonyms

SU5416
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (79)

All In Vivo ImagingIn Vivo Efficacy StudyCell Proliferation/Viability AssayHistological Imaging/StainingWB

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Journal Impact Factor

Adv Funct Mater

2021 May 24.
Circ Res

Endothelial FUNDC1 Deficiency Drives Pulmonary Hypertension. [Abstract]

2025 Jan 17;136(2):e1-e19. PMID: 39655444
Nat Commun

Clonal hematopoiesis with JAK2V617F promotes pulmonary hypertension with ALK1 upregulation in lung neutrophils. [Abstract]

2021 Oct 26;12(1):6177. PMID: 34702814
Int J Biol Macromol

5-Methylcytosine-modified circRNA-CCNL2 regulates vascular remdeling in hypoxic pulmonary hypertension through binding to FXR2. [Abstract]

2025 Jan 10:139638. PMID: 39800017
Int J Biol Macromol

Super enhancer-associated circRNA-circLrch3 regulates hypoxia-induced pulmonary arterial smooth muscle cells pyroptosis by formation of R-loop with host gene. [Abstract]

2024 May;268(Pt 2):130853. PMID: 38570000
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

Licochalcone B alleviates pulmonary vascular remodeling via inhibiting Furin/TGF-β1 in pulmonary hypertension. [Abstract]

2026 Aug:158:158373. PMID: 42263545
Phytomedicine

Baicalin attenuates pulmonary hypertension by targeting AMPK/CPT1A-mediated fatty acid metabolism. [Abstract]

2025 Dec 11:150:157703. PMID: 41447844
Phytomedicine

Typhae Pollen active subfraction exerts antiangiogenic effect in benign prostatic hyperplasia via regulating the VEGF signaling pathway and arachidonic acid metabolism. [Abstract]

2025 Nov:147:157237. PMID: 40934757

Semaxinib purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Nov:147:157237. [Abstract]

Representative images of zebrafish embryos at 24 hdf treated with SU5416 (2.5 μM) for 24 h using an inverted fluorescence microscope (n = 10). Defects in ISVs formation were marked with asterisks.

Semaxinib purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Nov:147:157237. [Abstract]

Cell viability of HUVECs treated with different concentrations of SU5416 (2.5 μM) for 24 h (n = 4).
Free Radic Biol Med

TRIB2 promotes pulmonary artery smooth muscle cell proliferation through SERCA2 ubiquitination in pulmonary hypertension. [Abstract]

2025 Nov 8:243:414-433. PMID: 41213438
Hypertension

Peptide Blocking Self-Polymerization of Extracellular Calcium-Sensing Receptor Attenuates Hypoxia-Induced Pulmonary Hypertension. [Abstract]

2021 Nov;78(5):1605-1616. PMID: 34565182
Br J Pharmacol

Established pulmonary hypertension in rats was reversed by a combination of a HIF-2α antagonist and a p53 agonist. [Abstract]

2022 Mar;179(5):1065-1081. PMID: 34599843
J Transl Med

From bench to bedside: elucidating VEGF(R) inhibitor-related heart failure in cancer treatment. [Abstract]

2025 Jan 23;23(1):109. PMID: 39849527
J Transl Med

Lactate dehydrogenase A (LDHA)-mediated lactate generation promotes pulmonary vascular remodeling in pulmonary hypertension. [Abstract]

2024 Aug 5;22(1):738. PMID: 39103838
Biomed Pharmacother

Post-treatment with Resolvin D1 attenuates pulmonary hypertension by inhibiting endothelial-to-mesenchymal transition. [Abstract]

2024 Jun 21:177:117023. PMID: 38908199
Biomed Pharmacother

Epigallocatechin-3-gallate inhibits tumor angiogenesis: involvement of endoglin/Smad1 signaling in human umbilical vein endothelium cells. [Abstract]

2019 Dec;120:109491. PMID: 31586903
Stem Cell Res Ther

DPSCs treated by TGF-β1 regulate angiogenic sprouting of three-dimensionally co-cultured HUVECs and DPSCs through VEGF-Ang-Tie2 signaling. [Abstract]

2021 May 10;12(1):281. PMID: 33971955
Cell Chem Biol

Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses. [Abstract]

2022 Jul 21;29(7):1113-1125.e6. PMID: 35728599
Antioxidants (Basel)

Effects of Bcl-2/Bcl-xL Inhibitors on Pulmonary Artery Smooth Muscle Cells. [Abstract]

2018 Oct 26;7(11). pii: E150. PMID: 30373097
Commun Med (Lond)

Insights from pharmacovigilance databases, clinical cohorts and preclinical models into VEGF(R) inhibitor-induced arthritis in cancer. [Abstract]

2025 Nov 18;5(1):478. PMID: 41254158
Comput Biol Med

Mechanistic study of ANXA3-mediated endoplasmic reticulum stress promoting M1 macrophage polarization in pulmonary arterial hypertension based on bioinformatics and nine machine learning algorithms. [Abstract]

2025 Oct 18;198(Pt B):111215. PMID: 41110296

Semaxinib purchased from MedChemExpress. Usage Cited in: Comput Biol Med. 2025 Oct 18;198(Pt B):111215. [Abstract]

Representative right ventricular pressure waveform in SuHx rats (a single subcutaneous injection of SU5416 at 20 mg/kg).

Semaxinib purchased from MedChemExpress. Usage Cited in: Comput Biol Med. 2025 Oct 18;198(Pt B):111215. [Abstract]

HE staining of pulmonary vessels in SuHx rats (a single subcutaneous injection of SU5416 at 20 mg/kg).

Semaxinib purchased from MedChemExpress. Usage Cited in: Comput Biol Med. 2025 Oct 18;198(Pt B):111215. [Abstract]

Quantitative analysis of RVEDD, RVEF and TAPSE in SuHx rats (a single subcutaneous injection of SU5416 at 20 mg/kg).
Cell Mol Life Sci

Rab26 promotes hypoxia-induced hyperproliferation of PASMCs by modulating the AT1R-STAT3-YAP axis. [Abstract]

2025 Nov 13;82(1):396. PMID: 41231254
Cancer Cell Int

Epidermal growth factor receptor ligands enriched in follicular fluid exosomes promote oncogenesis of fallopian tube epithelial cells. [Abstract]

2024 Dec 21;24(1):424. PMID: 39709453
Biochem Pharmacol

Scutellarein ameliorates pulmonary arterial hypertension via sirtuin 1 mediated deacetylation of nicotinamide nucleotide transhydrogenase. [Abstract]

2025 Apr 4:116932. PMID: 40189160
Chem Biol Interact

Mechanism of ferroptosis in hypoxia-induced pulmonary vascular remodeling in hypoxia pulmonary hypertension: a study based on the ACE2-Ang-(1-7)-Mas axis. [Abstract]

2025 Jun 2:111596. PMID: 40466901
J Ethnopharmacol

Ethyl cinnamate suppresses tumor growth through anti-angiogenesis by attenuating VEGFR2 signal pathway in colorectal cancer. [Abstract]

2024 May 23:326:117913. PMID: 38360380
Am J Respir Cell Mol Biol

Smooth Muscle Cell-Specific LKB1 Protects Against Sugen5416/Hypoxia-Induced Pulmonary Hypertension through Inhibition of BMP4. [Abstract]

2025 Feb;72(2):169-180. PMID: 39236291
Am J Respir Cell Mol Biol

Transplantation of Mesenchymal Stem Cells Attenuates Pulmonary Hypertension by Normalizing the Endothelial-to-Mesenchymal Transition. [Abstract]

2020 Jan;62(1):49-60. PMID: 31211918
J Am Heart Assoc

Ultrastructural Changes of the Right Ventricular Myocytes in Pulmonary Arterial Hypertension. [Abstract]

2019 Mar 5;8(5):e011227. PMID: 30807241
Drug Des Devel Ther

Ginsenoside Rg1 Ameliorates Pulmonary Hypertension by Inhibiting cGAS/STING Mediated Cell Senescence. [Abstract]

2025 Jul 29:19:6487-6504. PMID: 40756267
Respir Res

The P4HA1/HIF1α feedback loop modulates endothelial dysfunction in pulmonary hypertension. [Abstract]

2025 Nov 22;26(1):353. PMID: 41275293
Respir Res

Echocardiographic evaluation of right heart failure which might be associated with DNA damage response in SU5416-hypoxia induced pulmonary hypertension rat model. [Abstract]

2023 Aug 17;24(1):202. PMID: 37592245
Respir Res

Fibroblast growth factor 10 attenuates chronic obstructive pulmonary disease by protecting against glycocalyx impairment and endothelial apoptosis. [Abstract]

2022 Oct 1;23(1):269. PMID: 36183124
Int J Mol Sci

Metformin Preserves VE-Cadherin in Choroid Plexus and Attenuates Hydrocephalus via VEGF/VEGFR2/p-Src in an Intraventricular Hemorrhage Rat Model. [Abstract]

2022 Aug 2;23(15):8552. PMID: 35955686
Front Pharmacol

Combination Therapy With Rapamycin and Low Dose Imatinib in Pulmonary Hypertension. [Abstract]

2021 Nov 11;12:758763. PMID: 34858182
Front Pharmacol

Upregulation of IRF9 Contributes to Pulmonary Artery Smooth Muscle Cell Proliferation During Pulmonary Arterial Hypertension. [Abstract]

2021 Dec 1:12:773235. PMID: 34925032
J Mol Cell Cardiol

Extracellular-cAMP suppresses pulmonary arterial hypertension-induced ventricular arrhythmias. [Abstract]

2025 Dec 8:211:109-118. PMID: 41371472
Eur J Pharmacol

Phospholysine phosphohistidine inorganic pyrophosphate phosphatase suppresses glycolysis and proliferation of pulmonary artery smooth muscle cells in hypoxic pulmonary hypertension via inhibition of lactate dehydrogenase A. [Abstract]

2025 Sep 20:178172. PMID: 40983122
Eur J Pharmacol

The mechanism of the imbalance between proliferation and ferroptosis in pulmonary artery smooth muscle cells based on the activation of SLC7A11. [Abstract]

2022 Aug 5:928:175093. PMID: 35700835
Hypertens Res

A novel rat model of pulmonary hypertension induced by mono treatment with SU5416. [Abstract]

2020 Aug;43(8):754-764. PMID: 32472112
Transl Stroke Res

Inhibition of VEGF Signaling Reduces Diabetes-Exacerbated Brain Swelling, but Not Infarct Size, in Large Cerebral Infarction in Mice. [Abstract]

2018 Oct;9(5):540-548. PMID: 29290003
FASEB J

Echinatin Alleviates Experimental Pulmonary Hypertension by PPARγ Pathway Activation. [Abstract]

2026 Feb 15;40(3):e71542. PMID: 41631386
FASEB J

TRPV2 Inhibition Prevents Right Ventricular Remodeling and Arrhythmia in Experimental Pulmonary Hypertension. [Abstract]

2025 Aug 31;39(16):e70949. PMID: 40824146
J Cell Mol Med

Identification of LDHA as a Potential Therapeutic Target for Pulmonary Hypertension Through Modulation of Endothelial-To-Mesenchymal Transition. [Abstract]

2025 Jul;29(13):e70692. PMID: 40629253
FASEB J

Mitochondrial Genome-Encoded lncND5 Regulates Mitophagy in Hypoxic Pulmonary Artery Smooth Muscle Cell. [Abstract]

2025 May 31;39(10):e70618. PMID: 40364724
J Cell Mol Med

High expression of DEC2 distinguishes chondroblastic osteosarcoma and promotes tumour growth by activating the VEGFC/VEGFR2 signalling pathway. [Abstract]

2024 Jun;28(11):e18462. PMID: 38847478
Environ Toxicol Pharmacol

Effects of cooking oil fume derived fine particulate matter on blood vessel formation through the VEGF/VEGFR2/MEK1/2/ERK1/2/mTOR pathway in human umbilical vein endothelial cells. [Abstract]

2019 Jul:69:112-119. PMID: 31026735
Am J Physiol Heart Circ Physiol

Non-invasive surrogate of main pulmonary artery stiffness is associated with right ventricular function in experimental pulmonary arterial hypertension. [Abstract]

2026 Jun 11. PMID: 42275165
Cell Calcium

TRPV2 inhibitor tranilast prevents atrial fibrillation in rat models of pulmonary hypertension. [Abstract]

2024 Jan:117:102840. PMID: 38160478
Cell Signal

TG2 participates in pulmonary vascular remodelling by regulating the senescence of pulmonary artery smooth muscle cells. [Abstract]

2024 Jul 14:121:111296. PMID: 39009200
Cell Signal

Ligand-mediated dephosphorylation signaling for MAP kinase. [Abstract]

2018 Dec:52:147-154. PMID: 30213686
Am J Pathol

Increased Smooth Muscle Kv11.1 Channel Expression in Pulmonary Hypertension and Protective Role of Kv11.1 Channel Blocker Dofetilide. [Abstract]

2020 Jan;190(1):48-56. PMID: 31839145
Clin Exp Hypertens

Cinnamaldehyde alleviates pulmonary hypertension by affecting vascular remodeling through the TLR4/NF-kB/HIF-1a pathway. [Abstract]

2025 Dec;47(1):2486829. PMID: 40171680
Pathol Res Pract

LGALS3BP promotes M1 polarization of macrophages and interacts with LGALS3, damaging endothelial function and exacerbating pulmonary arterial hypertension in systemic lupus erythematosus. [Abstract]

2026 Jun:282:156424. PMID: 41791134
Curr Issues Mol Biol

Brain-Derived Cystathionine β-Synthase-Generated H2S Attenuates Cerebral Ischemia-Reperfusion Injury via VEGFR2-Mediated Angiogenesis in MCAO/R Rats. [Abstract]

2026 Apr 18;48(4):418. PMID: 42042078
Genomics

Upregulation of the key biomarker kinesin family member 20A (KIF20A) is associated with pulmonary artery hypertension. [Abstract]

2023 Sep 12;115(5):110705. PMID: 37703933
Front Cardiovasc Med

Metabolic Reprogramming in the Heart and Lung in a Murine Model of Pulmonary Arterial Hypertension. [Abstract]

2018 Aug 15:5:110. PMID: 30159317
Microvasc Res

VEGFR2 in vascular smooth muscle cells mediates H2S-induced dilation of the rat cerebral basilar artery. [Abstract]

2022 May:141:104309. PMID: 34995553
BMC Anesthesiol

Propofol attenuated TNF-α-modulated occludin expression by inhibiting Hif-1α/ VEGF/ VEGFR-2/ ERK signaling pathway in hCMEC/D3 cells. [Abstract]

2019 Jul 9;19(1):127. PMID: 31288745

Semaxinib purchased from MedChemExpress. Usage Cited in: BMC Anesthesiol. 2019 Jul 9;19(1):127. [Abstract]

The hCMEC/D3 cells are incubated with TNF-α and VEGFR-2 inhibitor (SU5416, 10 μM). Left side shows the image of a representative Western blot for VEGF, p-VEGFR-2, p-ERK, ERK and occludin in hCMEC/D3 cells. Right side is the plot of normalized ratios of optical densities. β-actin is served as internal loading control.
BMC Cardiovasc Disord

Prognostic significance of circulating level of GRP78 in pulmonary arterial hypertension. [Abstract]

2026 Apr 29;26(1):513. PMID: 42056874
J Recept Signal Transduct Res

Effect of elastin on abnormal proliferation of pulmonary artery smooth muscle cells at an early stage of hypoxic exposure. [Abstract]

2024 Nov 26:1-11. PMID: 39587908
J Mol Cell Cardiol Plus

The selective serotonin reuptake inhibitor paroxetine improves right ventricular systolic function in experimental pulmonary hypertension. [Abstract]

2024 Mar 26:8:100072. PMID: 39802918
Physiol Rep

Oral administration of pioglitazone inhibits pulmonary hypertension by regulating the gut microbiome and plasma metabolome in male rats. [Abstract]

2025 Jan;13(1):e70174. PMID: 39739369
Physiol Rep

Modulation of soluble guanylate cyclase ameliorates pulmonary hypertension in a rat model of chronic thromboembolic pulmonary hypertension by stimulating angiogenesis. [Abstract]

2022 Jan;10(1):e15156. PMID: 35001565
Transplant Proc

Tirofiban Promotes the Proliferation of Human Umbilical Vein Endothelial Cells In Vitro Via Enhanced Vascular Endothelial Growth Factor Expression. [Abstract]

Jan-Feb 2020;52(1):419-422. PMID: 31948801
bioRxiv

2026 Mar 9.
SSRN

2026 Mar 29.
bioRxiv

Sotatercept Reverses SIN3a Deficiency-Driven PAH by Reprogramming BMPR2/TGF-β-HIF-1α Signaling Pathways. [Abstract]

2026 Feb 3:2026.02.03.703590. PMID: 41676700
bioRxiv

Tau seeding in neurons enabled by transient endolysosomal perforations are confined within endolysosomes. [Abstract]

2025 Nov 3:2025.11.02.686178. PMID: 41278722
bioRxiv

Bidirectional Crosstalk Between Sleep and Pulmonary Arterial Hypertension. [Abstract]

2025 Jul 27:2025.07.23.666314. PMID: 40777305
bioRxiv

Paracrine Action of Bone Morphogenetic Protein 3 in Pulmonary Arterial Hypertension. [Abstract]

2025 Jun 18:2025.06.13.659638. PMID: 40666946
SSRN

2025 May 18.
bioRxiv

2025 April 16.
bioRxiv

2024 May 10.
bioRxiv

VEGFA mRNA-LNP promotes biliary epithelial cell-to-hepatocyte conversion in acute and chronic liver diseases and reverses steatosis and fibrosis. [Abstract]

2023 Apr 18:2023.04.17.537186. PMID: 37131823
Methods Mol Biol

Intra-Airway Gene Delivery for Pulmonary Hypertension in Rodent Models. [Abstract]

2022;2573:263-278. PMID: 36040601
Oxid Med Cell Longev

Artemisinin and Its Derivate Alleviate Pulmonary Hypertension and Vasoconstriction in Rodent Models. [Abstract]

2022 Jun 17:2022:2782429. PMID: 35757500
Research Square Preprint

2021 Oct.
Research Square Preprint

2021 Feb.

Solvant et solubilité

In Vitro:

DMF : 50 mg/mL (209.84 mM; Need ultrasonic)

DMSO : 10 mg/mL (41.97 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.1967 mL

20.9837 mL

41.9674 mL

5 mM

0.8393 mL

4.1967 mL

8.3935 mL

10 mM

0.4197 mL

2.0984 mL

4.1967 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (10.49 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.25 mg/mL (9.44 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.25 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 (22.5 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocole

Cell Assay

3T3Her2 and 488G2M2 are NIH3T3 fibroblast cell lines engineered to overexpress Her2 and to express human PDGF-BB and human PDGF receptor β. Both cell lines are cultured in DMEM supplemented with 2% CS and 2 mM L-glutamine. C6, Calu 6, A375, A431, and SF767T are plated in their respective growth medium at 2×10³ cells/100 μL/well in 96-well, flat-bottomed plates. Semaxinib (SU5416) is serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth is measured after 96 h using the sulforhodamine B method. IC₅₀s are calculated by curve fitting using four-parameter analysis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]^[3]

Mice^[1]
Female BALB/c nu/nu mice (20-22 g; 12 weeks of age) are used. Aseptic technique is used during this surgical procedure. A small midline incision (1 cm) is made in the abdomen directly over the colon. C6 cells are implanted (0.5×10⁶ cells/animal) under the serosa of the colon using a 27-gauge needle. After implantation, all exposed sections of the intestine are returned into the abdominal cavity. The peritoneum and skin are closed using a 6.0 surgical suture and wound clips. The wound clips are removed 7 days after surgery. Animals are treated once daily with a 50 μL i.p. bolus injection of either Semaxinib (SU5416) or DMSO, beginning 1 day after implantation. Approximately 13-16 days after implantation, animals are euthanized, and local tumor growth on the colon is quantitated either by weighing the tumors or by measuring the tumors using venier calipers. Tumor volumes are calculated as the product of length×width×height.
Rats^[3]
Male Sprague Dawley rats (n=60, 6-8 wk) are randomly divided among five groups: control (Con), Semaxinib (SU), pneumonectomy (PNx), Semaxinib+hypoxia (SuHx), and Semaxinib+PNx (SuPNx). The SuHx protocol is employed. Briefly, animals are injected with Semaxinib (25 mg/kg) dissolved in carboxymethylcellulose (CMC) and exposed to hypoxia (10%) for 4 wk followed by re-exposure to normoxia. PNx animals underwent a left pneumonectomy. Two days following PNx surgery an injection of Semaxinib is administered (25 mg/kg). The Con group received only the solvent CMC. Echocardiography is utilized at baseline (prehypoxia/presurgery), week 2, and week 6 to determine cardiac morphometry and function. Two and six weeks postsurgery/posthypoxia animals are anesthetized and right ventricle (RV) and left ventricle (LV) pressure measurements via catheterization are performed.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (285 KB)
SDS (396 KB)
- English - EN (396 KB)
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- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Fong TA, et al. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res, 1999, 59(1), 99-106. [Content Brief]

[2]. Vajkoczy P, et al. Inhibition of tumor growth, angiogenesis, and microcirculation by the novel Flk-1 inhibitor SU5416 as assessed by intravital multi-fluorescence videomicroscopy. Neoplasia, 1999, 1(1), 31-41. [Content Brief]

[3]. Happé CM, et al. Pneumonectomy combined with SU5416 induces severe pulmonary hypertension in rats.Am J Physiol Lung Cell Mol Physiol. 2016 Jun 1;310(11):L1088-97. [Content Brief]

[4]. Izquierdo-Garcia JL, et al. Metabolic Reprogramming in the Heart and Lung in a Murine Model of Pulmonary Arterial Hypertension. Front Cardiovasc Med. 2018 Aug 15;5:110. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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 / DMF	1 mM	4.1967 mL	20.9837 mL	41.9674 mL	104.9186 mL
	5 mM	0.8393 mL	4.1967 mL	8.3935 mL	20.9837 mL
	10 mM	0.4197 mL	2.0984 mL	4.1967 mL	10.4919 mL
	15 mM	0.2798 mL	1.3989 mL	2.7978 mL	6.9946 mL
	20 mM	0.2098 mL	1.0492 mL	2.0984 mL	5.2459 mL
	25 mM	0.1679 mL	0.8393 mL	1.6787 mL	4.1967 mL
	30 mM	0.1399 mL	0.6995 mL	1.3989 mL	3.4973 mL
	40 mM	0.1049 mL	0.5246 mL	1.0492 mL	2.6230 mL
DMF	50 mM	0.0839 mL	0.4197 mL	0.8393 mL	2.0984 mL
	60 mM	0.0699 mL	0.3497 mL	0.6995 mL	1.7486 mL
	80 mM	0.0525 mL	0.2623 mL	0.5246 mL	1.3115 mL
	100 mM	0.0420 mL	0.2098 mL	0.4197 mL	1.0492 mL

Keywords

Semaxinib

79 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Semaxinib

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Chemical Information

Publications (79)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Semaxinib Related Classifications

HY-10374 Related Classifications