Semaxinib (Synonyms: SU5416)

Name: Semaxinib
Brand: MedChemExpress
SKU: HY-10374
Rating: 5.0 (74 reviews)

Cat. No.: HY-10374 Purity: 99.92%: Data Sheet
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Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC₅₀ of 1.23 μM.

For research use only. We do not sell to patients.

CAS No. : 204005-46-9

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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 74 publication(s) in Google Scholar

Other Forms of Semaxinib:

(Z)-Semaxanib In-stock
Semaxinib (Standard) Get quote

74 Publications Citing Use of MCE Semaxinib

In Vivo Imaging

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

Histological Imaging/Staining

: 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).

: 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).

: 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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)

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]
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: 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	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	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]
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]
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]
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]
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]
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.

Clinical Trial

Molecular Weight

238.28

Formula

C₁₅H₁₄N₂O

CAS No.

204005-46-9

Appearance

Solid

Color

Brown to orange

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (285 KB) SDS (396 KB)

COA (254 KB) LCMS (111 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Semaxinib Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Semaxinib204005-46-9SU5416SU 5416SU-5416VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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Semaxinib (Synonyms: SU5416)

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