2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. KGP591

KGP591 is a tubulin polymerization inhibitor (IC50 0.57 µM). KGP591 induces significant G2/M stagnation, inhibits cell migration, disrupts microtubule structure and cell morphology in MDA-MB-231 cells. KGP591 shows antitumor activity in orthotopic model of kidney cancer (RENCA).

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KGP591

KGP591 Chemical Structure

CAS No. : 3018962-69-8

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KGP591 Related Antibodies

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Description

KGP591 is a tubulin polymerization inhibitor (IC50 0.57 µM). KGP591 induces significant G2/M stagnation, inhibits cell migration, disrupts microtubule structure and cell morphology in MDA-MB-231 cells. KGP591 shows antitumor activity in orthotopic model of kidney cancer (RENCA)[1].

In Vitro

KGP591 (100 nM, 72 h) inhibits migration and proliferation in MDA-MB-231 cells [1]>.
KGP591 (100 nM, 30 min) induces microtubule disruption in MDA-MB-231 cells[1].
KGP591 (200 nM, 48 h) shows G2/M cell cycle arrest in MDA-MB-231 cells[1].

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

KGP591 Related Antibodies

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells
Concentration: 100 nM
Incubation Time: 72 h
Result: Decreased in wound width in cells and remained largely open.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 200 nM
Incubation Time: 48 h
Result: Had an arrest of MDA-MB-231 cells at G2/M of the cell cycle.
In Vivo

Phosphate prodrug KGP618 (150 mg/kg, subcutaneous injection, 24 h) for KGP591 shows tumor-selective vascular disrupting agents (VDA) efficacy in BALB/c mice with RENCA-luc xenograft[1].

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

Animal Model: RENCA-luc xenograft in BALB/c mice[1]
Dosage: 150 mg/kg
Administration: Subcutaneous Injection
Result: Caused significant reduction of Bio-Layer Interferometry (BLI) signal occurred within 2.5 h.
Showed necrosis and severe hemorrhage in RENCA tumor tissue.
Molecular Weight

403.43

Formula

C24H21NO5
CAS No.
SMILES

COC1=CC(C(C2=CNC3=CC(C4=CC=CC(O)=C4)=CC=C23)=O)=CC(OC)=C1OC
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Room temperature in continental US; may vary elsewhere.
Storage

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

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    Tubulin polymerization was evaluated in 0.25 mL reaction mixtures (final volume) containing 1 mg/mL (10 μM) purified bovine brain tubulin, 0.8 M monosodium glutamate (pH 6.6), 4% (v/v) DMSO, 0.1 mM GTP.

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Purity & Documentation
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KGP591 Related Classifications

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:

KGP5913018962-69-8KGP 591KGP-591Microtubule/TubulinMDA-MB-231 cellinhibitors of Tubulin PolymerizationBALB/c micecancerbreast cancerkidney cancerRENCAInhibitorinhibitorinhibit

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