1. Vitamin D Related/Nuclear Receptor Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  2. Estrogen Receptor/ERR Microtubule/Tubulin Apoptosis
  3. STX140

STX140 is an orally active microtubule disruptor. STX140 induces apoptosis in the hormone-independent PC-3 prostate cell lines. STX140 has anti-angiogenic and anti-tumour activities.

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STX140

STX140 Chemical Structure

CAS No. : 401600-86-0

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Description

STX140 is an orally active microtubule disruptor. STX140 induces apoptosis in the hormone-independent PC-3 prostate cell lines. STX140 has anti-angiogenic and anti-tumour activities[1].

Cellular Effect
Cell Line Type Value Description References
DU-145 GI50
0.083 μM
Compound: 21, 2-MeOE2bisMATE
Growth inhibition of human DU145 cell line
Growth inhibition of human DU145 cell line
[PMID: 17181151]
DU-145 GI50
0.34 μM
Compound: 2
Antiproliferative activity against human DU145 cells after 96 hrs by WST-1 assay
Antiproliferative activity against human DU145 cells after 96 hrs by WST-1 assay
[PMID: 20225862]
DU-145 GI50
0.34 μM
Compound: 3
Antiproliferative activity against human DU145 cells after 96 hrs by WST1 assay
Antiproliferative activity against human DU145 cells after 96 hrs by WST1 assay
[PMID: 17696419]
DU-145 GI50
0.34 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against human DU145 cells
Antiproliferative activity against human DU145 cells
[PMID: 18260615]
HCT-116 GI50
0.045 μM
Compound: 2
Antiproliferative activity against human HCT116 cells after 96 hrs by WST-1 assay
Antiproliferative activity against human HCT116 cells after 96 hrs by WST-1 assay
[PMID: 20225862]
HCT-116 GI50
0.045 μM
Compound: 21, 2-MeOE2bisMATE
Growth inhibition of human HCT116 cell line
Growth inhibition of human HCT116 cell line
[PMID: 17181151]
HCT-116 GI50
0.045 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against human HCT116 cells
Antiproliferative activity against human HCT116 cells
[PMID: 18260615]
HOP-62 GI50
0.051 μM
Compound: 2
Antiproliferative activity against human HOP62 cells after 96 hrs by WST-1 assay
Antiproliferative activity against human HOP62 cells after 96 hrs by WST-1 assay
[PMID: 20225862]
HOP-62 GI50
0.051 μM
Compound: 21, 2-MeOE2bisMATE
Growth inhibition of human HOP62 cell line
Growth inhibition of human HOP62 cell line
[PMID: 17181151]
HOP-62 GI50
0.051 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against human HOP62 cells
Antiproliferative activity against human HOP62 cells
[PMID: 18260615]
HUVEC IC50
0.13 μM
Compound: 21, 2-MeOE2bisMATE
Antiangiogenic activity assessed as inhibition of cord formation in HUVEC
Antiangiogenic activity assessed as inhibition of cord formation in HUVEC
[PMID: 17181151]
HUVEC IC50
0.4 μM
Compound: 21, 2-MeOE2bisMATE
Antiangiogenic activity in HUVEC by chemotaxis assay
Antiangiogenic activity in HUVEC by chemotaxis assay
[PMID: 17181151]
HUVEC IC50
0.7 μM
Compound: 21, 2-MeOE2bisMATE
Antiangiogenic activity assessed as growth inhibition in HUVEC
Antiangiogenic activity assessed as growth inhibition in HUVEC
[PMID: 17181151]
HUVEC IC50
44 nM
Compound: 3, 2-MeO2bisMATE
Antiangiogenic activity against HUVEC cells assessed as inhibition of proliferation
Antiangiogenic activity against HUVEC cells assessed as inhibition of proliferation
[PMID: 18260615]
MCF7 GI50
0.25 μM
Compound: 21, 2-MeOE2bisMATE
Antiproliferative activity against human MCF7 cell line
Antiproliferative activity against human MCF7 cell line
[PMID: 17181151]
MCF7 GI50
0.25 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against estrogen receptor positive human MCF7 cells
Antiproliferative activity against estrogen receptor positive human MCF7 cells
[PMID: 18260615]
MCF7 IC50
0.25 μM
Compound: 15
Antiproliferative activity against estrogen receptor-positive human MCF7 cells
Antiproliferative activity against estrogen receptor-positive human MCF7 cells
[PMID: 31255926]
MDA-MB-231 ED50
10 mg/kg
Compound: 43
Antitumor activity against human MDA-MB-231 cells xenografted in MF1 mouse administered daily
Antitumor activity against human MDA-MB-231 cells xenografted in MF1 mouse administered daily
[PMID: 25992880]
MDA-MB-231 ED50
20 mg/kg
Compound: 43
Antitumor activity against human MDA-MB-231 cells xenografted in MF1 mouse administered thrice weekly
Antitumor activity against human MDA-MB-231 cells xenografted in MF1 mouse administered thrice weekly
[PMID: 25992880]
MDA-MB-231 GI50
0.28 μM
Compound: 2
Antiproliferative activity against human MDA-MB-231 cells after 96 hrs by WST-1 assay
Antiproliferative activity against human MDA-MB-231 cells after 96 hrs by WST-1 assay
[PMID: 20225862]
MDA-MB-231 GI50
0.28 μM
Compound: 3
Antiproliferative activity against human MDA-MB-231 cells after 96 hrs by WST1 assay
Antiproliferative activity against human MDA-MB-231 cells after 96 hrs by WST1 assay
[PMID: 17696419]
MDA-MB-231 GI50
0.28 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against estrogen receptor negative human MDA-MB-231 cells
Antiproliferative activity against estrogen receptor negative human MDA-MB-231 cells
[PMID: 18260615]
MDA-MB-231 IC50
0.29 μM
Compound: 15
Antiproliferative activity against estrogen receptor-negative human MDA-MB-231 cells
Antiproliferative activity against estrogen receptor-negative human MDA-MB-231 cells
[PMID: 31255926]
MDA-MB-435 GI50
< 0.01 μM
Compound: 21, 2-MeOE2bisMATE
Growth inhibition of human MDA-MB-435 cell line
Growth inhibition of human MDA-MB-435 cell line
[PMID: 17181151]
MDA-MB-435 GI50
< 0.01 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against human MDA-MB-435 cells
Antiproliferative activity against human MDA-MB-435 cells
[PMID: 18260615]
OVCAR-3 GI50
< 0.01 μM
Compound: 2
Antiproliferative activity against human OVCAR-3 cells after 96 hrs by WST-1 assay
Antiproliferative activity against human OVCAR-3 cells after 96 hrs by WST-1 assay
[PMID: 20225862]
OVCAR-3 GI50
< 0.01 μM
Compound: 21, 2-MeOE2bisMATE
Growth inhibition of human OVCAR-3 cell line
Growth inhibition of human OVCAR-3 cell line
[PMID: 17181151]
OVCAR-3 GI50
< 0.01 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against human OVCAR-3 cells
Antiproliferative activity against human OVCAR-3 cells
[PMID: 18260615]
SF-539 GI50
0.036 μM
Compound: 2
Antiproliferative activity against human SF539 cells after 96 hrs by WST-1 assay
Antiproliferative activity against human SF539 cells after 96 hrs by WST-1 assay
[PMID: 20225862]
SF-539 GI50
0.036 μM
Compound: 21, 2-MeOE2bisMATE
Growth inhibition of human SF539 cell line
Growth inhibition of human SF539 cell line
[PMID: 17181151]
SF-539 GI50
0.036 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against human SF539 cells at
Antiproliferative activity against human SF539 cells at
[PMID: 18260615]
SN12C GI50
0.126 μM
Compound: 2
Antiproliferative activity against human SN12C cells after 96 hrs by WST-1 assay
Antiproliferative activity against human SN12C cells after 96 hrs by WST-1 assay
[PMID: 20225862]
SN12C GI50
0.126 μM
Compound: 21, 2-MeOE2bisMATE
Growth inhibition of human SN12-C cell line
Growth inhibition of human SN12-C cell line
[PMID: 17181151]
SN12C GI50
0.126 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against human SN12-C cells
Antiproliferative activity against human SN12-C cells
[PMID: 18260615]
UACC-62 GI50
< 0.01 μM
Compound: 2
Antiproliferative activity against human UACC62 cells after 96 hrs by WST-1 assay
Antiproliferative activity against human UACC62 cells after 96 hrs by WST-1 assay
[PMID: 20225862]
UACC-62 GI50
< 0.01 μM
Compound: 21, 2-MeOE2bisMATE
Growth inhibition of human UACC62 cell line
Growth inhibition of human UACC62 cell line
[PMID: 17181151]
UACC-62 GI50
< 0.01 μM
Compound: 3, 2-MeO2bisMATE
Antiproliferative activity against human UACC62 cells
Antiproliferative activity against human UACC62 cells
[PMID: 18260615]
In Vitro

STX140 is a potent inhibitor of cell proliferation in a panel of prostate and breast cancer cell lines, with IC50 values of 270 nM, 290 nM, 260 nM, 250 nM, 280 nM, and 44 nM for PC-3, MDA-MB-231, LNCaP, MCF-7, A2780, and HUVEC, respectively[1].
STX140 (0.5 μM; 24 h) potently induces cell cycle arrest. STX140 induces apoptosis in the hormone-independent PC-3 prostate cell line[1].

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

Cell Cycle Analysis[1]

Cell Line: PC-3 cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Potently induced cell cycle arrest with 71% of PC-3 cells being in G2/M after 24 h and 6% in G1.
In Vivo

STX140 (20 mg/kg; p.o.; once daily; 60 days) leads to tumour regression and complete responses, which are maintained after the cessation of dosing[1].

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

Animal Model: Male MF-1 nu/nu mice injected with PC-3 cells[1]
Dosage: 20 mg/kg
Administration: p.o.; once daily; 60 days
Result: Led to tumour regression and complete responses.
Molecular Weight

460.56

Formula

C19H28N2O7S2

CAS No.
SMILES

C[C@@]12[C@](CC[C@@H]2OS(N)(=O)=O)([H])[C@@]3([H])[C@@](CC1)([H])C4=CC(OC)=C(OS(N)(=O)=O)C=C4CC3

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
References
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STX140
Cat. No.:
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