1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. E7130

E7130 is a microtubule inhibitor, which ameliorates the tumor microenvironment through suppression of cancer-associated fibroblasts (CAF) and promotion of tumor vasculature remodeling.

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

E7130 Chemical Structure

E7130 Chemical Structure

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Description

E7130 is a microtubule inhibitor, which ameliorates the tumor microenvironment through suppression of cancer-associated fibroblasts (CAF) and promotion of tumor vasculature remodeling[1].

In Vitro

E7130 inhibits microtubule dynamics and exhibits anti-proliferative efficacy in cancer cells KPL-4, OSC-19, FaDu and HSC-2, with IC50s of 0.01-0.1 nM[1].
E7130 (0.15 nM) inihibits TGF-β-induced myofibroblast transdifferentiation through disruption of microtubule network formation, and thereby deactivates the PI3K/AKT/mTOR pathway[1].

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

Immunofluorescence[1]

Cell Line: BJ cells
Concentration: 0.15 nM
Incubation Time: 48 h
Result: Inhibited TGF-β-induced α-SMA expression in BJ cells without growth inhibitory activity.

Western Blot Analysis[1]

Cell Line: BJ cells
Concentration: 0.15 nM
Incubation Time: 48 h
Result: Decreased levels of pAKT and pS6.
In Vivo

E7130 (45-180 μg/kg, i.v.) increases the intratumoural microvessel density (MVD) and thereby increases the delivery of cetuximab (CTX) into tumors, causing a tumour regression in HSC-2 SCCHN xenograft BALB/c mice[1].
E7130 (45-180 μg/kg, i.v.) reduces the α-SMA-positive CAFs, the E7130-CTX combination modulates the phenotypes of the fibroblasts in FaDu SCCHN xenograft BALB/c mice[1].

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

Animal Model: FaDu SCCHN xenograft BALB/c mice[1]
Dosage: 45-180 μg/kg
Administration: i.v.
Result: Reduced the α-SMA-positive CAFs, modulated the phenotypes of the fibroblasts with combination of CTX.
Animal Model: HSC-2 SCCHN xenograft BALB/c mice[1]
Dosage: 90 μg/kg
Administration: i.v.
Result: Increased MVD, inhibited tumor growth.
Increased survival rate with combination of CTX.
Molecular Weight

1066.28

Formula

C58H83NO17

SMILES

O=C(C[C@@H]1O[C@@]([C@H](O[C@]2(CC3)O[C@H]4[C@H]5C2)[C@H](O5)[C@@]4([H])O6)([H])[C@]6([H])CC1)O[C@H]([C@H]7C)[C@H](C[C@H]8O[C@@H](CC[C@H]9C(C[C@@H]3O9)=C)C[C@@H](C)C8=C)O[C@@]([C@@]7([H])O%10)([H])C[C@@]([C@@]%10([H])C%11)([H])O[C@@]%11(O%12)C[C@]([C@]%12([H])[C@@H](C)C%13)([H])O[C@@]%14%13C[C@H](C)[C@]%15([H])O[C@H](CN)[C@H](O)C[C@]%15([H])O%14

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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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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E7130
Cat. No.:
HY-161248
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