1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. (Z)-Semaxanib

(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

(Z)-Semaxanib Chemical Structure

CAS No. : 194413-58-6

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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.
SMILES

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

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Storage

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

Purity & Documentation
References
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    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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(Z)-Semaxanib
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