(Z)-Semaxanib (Synonyms: (Z)-SU5416)

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(Z)-Semaxanib (compound (z)-1) is a potent tyrosine kinase inhibitor. (Z)-Semaxanib shows cytotoxicity for TAMH and HepG2 cells with IC₅₀s of 6.28 µM and 8.17 µM, respectively.

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(Z)-Semaxanib Chemical Structure

CAS No. : 194413-58-6

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Other Forms of (Z)-Semaxanib:

Semaxinib In-stock

2 Publications Citing Use of MCE (Z)-Semaxanib

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Description

(Z)-Semaxanib (compound (z)-1) is a potent tyrosine kinase inhibitor. (Z)-Semaxanib shows cytotoxicity for TAMH and HepG2 cells with IC₅₀s of 6.28 µM and 8.17 µM, respectively^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
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	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	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]
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]
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]
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	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]
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	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	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	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 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]
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]
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	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: 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 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	12.9 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 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 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	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	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]

Molecular Weight

238.29

Formula

C₁₅H₁₄N₂O

CAS No.

194413-58-6

SMILES

O=C(NC1=C/2C=CC=C1)C2=C/C3=C(C)C=C(C)N3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ngai MH, So CL, Sullivan MB, Ho HK, Chai CL. Photoinduced Isomerization and Hepatoxicities of Semaxanib, Sunitinib and Related 3-Substituted Indolin-2-ones. ChemMedChem. 2016 Jan 5;11(1):72-80. [Content Brief]

(Z)-Semaxanib Related Classifications

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Help & FAQs

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.

Keywords:

(Z)-Semaxanib194413-58-6(Z)-SU5416c-Met/HGFRTAMH cellsHepG2 cellscytotoxicityInhibitorinhibitorinhibit

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