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Art. -Nr.: HY-155249

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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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CAS. Nr.: 3018962-69-8
Formel: C₂₄H₂₁NO₅
Molecular Weight:403.43

Speicherung:

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

Data Sheet (276 KB)

KGP591 Chemical Structure

CAS. Nr.: 3018962-69-8

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vivo
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	GI₅₀	320 nM Compound: KGP591	Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by SRB assay Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 37984295]
MDA-MB-231	GI₅₀	102 nM Compound: KGP591	Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by SRB assay Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by SRB assay	[PMID: 37984295]

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.

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.

Chemical Information

CAS. Nr. 3018962-69-8
Molecular Weight 403.43
Formel C₂₄H₂₁NO₅
SMILES

COC1=CC(C(C2=CNC3=CC(C4=CC=CC(O)=C4)=CC=C23)=O)=CC(OC)=C1OC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Lösungsmittel & Löslichkeit

View the Complete Stock Solution Preparation Table

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Maguire CJ, et al. Synthesis and biological evaluation of structurally diverse α-conformationally restricted chalcones and related analogues. Medchemcomm. 2019 Jun 4;10(8):1445-1456. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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