Art. -Nr.: HY-10498

Lexibulin

(Synonyms: CYT-997)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells.

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Reinheit: 99.10%
CAS. Nr.: 917111-44-5
Formel: C₂₄H₃₀N₆O₂
Molecular Weight:434.53

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Lexibulin Chemical Structure

CAS. Nr.: 917111-44-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo^[1]^[2]. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells^[3].

IC₅₀ & Target

IC50 value: 10-100 nM(cell assay)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	338 nM Compound: 12, CYT997	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 24160376]
DU-145	IC₅₀	0.06 μM Compound: 24, CYT997	Cytotoxicity against human DU145 cells after 72 hrs by MTT assay Cytotoxicity against human DU145 cells after 72 hrs by MTT assay	[PMID: 19616947]
HCT-116	IC₅₀	356 nM Compound: 12, CYT997	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 24160376]
HL-60	IC₅₀	112.3 nM Compound: 12, CYT997	Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 24160376]
HUVEC	GI₅₀	2098 ng/mL Compound: 12, CYT997	Toxicity in HUVEC assessed as growth inhibition Toxicity in HUVEC assessed as growth inhibition	[PMID: 24160376]
NCI-H460	IC₅₀	272 nM Compound: 12, CYT997	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 24160376]
PC-3	IC₅₀	0.06 μM Compound: 24, CYT997	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 19616947]

In Vitro

Lexibulin (CYT-997) prevents the in vitro polymerization of tubulin with an IC50 of ～3 μmol/L (compared with the half-maximal inhibitory concentration of 2 μmol/L for colchicine under identical conditions) as determined using the conventional turbidimetric assay for tubulin polymerization. Lexibulin is also capable of reversibly disrupting the microtubule network in cells, visualized using fluorescence microscopy. Thus, treatment of A549 cells with Lexibulin (1 μM) lead to the rapid reorganization of microtubules, including the destruction of the existing microtubule network and accumulation of tubulin in plaques within the cytoplasm of some cells. After 24 hours, major alterations in cell morphology are evident, including loss of adhesion and cell rounding. The effect of 1 hour of treatment with Lexibulin is reversible and cells rapidly recovered their normal microtubule architecture. Taken together, the data indicates that Lexibulin belongs to the class of anticancer agents that disrupt, rather than stabilize, tubulin-containing structures. Although vehicle-treated cells show 15% and 19% in G2-M phase at 15 and 24 hours (respectively), cells treated with Lexibulin (1 μM) had 38% and 43% of cells in G2-M at the same time points. Furthermore, at 24 hours post-Lexibulin treatment, only 66% of total cells are in the G1, S, and G2-M phases, which suggests that cells blocked at the G2-M boundary do not exit back to G1, as in the normal cell cycle, but most likely are driven towards apoptosis and cell death^[1]. Consistent with the disruption of cellular tubulin, Lexibulin potently inhibits proliferation, induces cell cycle arrest and most importantly apoptosis of both human myeloma cell lines (HMCLs) and primary MM cells^[2].

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

In Vivo

iIn a xenograft model using the human prostate cancer cell line PC3, oral dosing of Lexibulin (CYT-997) is initiated 13 days after cell implantation by which time palpable tumors were evident. A dose-dependent inhibition of tumor growth was apparent with Lexibulin (CYT-997), which at the highest dose was equivalent to parenterally administered paclitaxel. A single dose of Lexibulin (CYT-997) (7.5 mg/kg i.p.) clearly decreased blood flow in liver metastases, and a significant reduction in blood flow was present 6 hours postdose^[1]. Lexibulin (CYT-997) treatment (15 mg/kg/day) significantly prolongs the survival in a murine model of aggressive systemic myelomatosis^[2].

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

Chemical Information

CAS. Nr. 917111-44-5
Appearance Solid
Molecular Weight 434.53
Formel C₂₄H₃₀N₆O₂
Color White to off-white
SMILES

CCC[C@H](NC1=C(C)C=NC(C2=CC=C(NC(NCC)=O)C(OC)=C2)=N1)C3=CN=CC=C3
Synonyms

CYT-997
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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J Exp Clin Cancer Res

Mitochondrial ROS accumulation inhibiting JAK2/STAT3 pathway is a critical modulator of CYT997-induced autophagy and apoptosis in gastric cancer. [Abstract]

2020 Jun 23;39(1):119. PMID: 32576206
bioRxiv

2024 Jul 25.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (230.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3013 mL

11.5067 mL

23.0134 mL

5 mM

0.4603 mL

2.3013 mL

4.6027 mL

10 mM

0.2301 mL

1.1507 mL

2.3013 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Burns CJ, et al. CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Mol Cancer Ther. 2009 Nov;8(11):3036-45. [Content Brief]

[2]. Monaghan K, et al. CYT997 causes apoptosis in human multiple myeloma. Invest New Drugs. 2011 Apr;29(2):232-8. [Content Brief]

[3]. Ya Cao, wt al. Mitochondrial ROS Accumulation Inhibiting JAK2/STAT3 Pathway Is a Critical Modulator of CYT997-induced Autophagy and Apoptosis in Gastric Cancer. J Exp Clin Cancer Res. 2020 Jun 23;39(1):119. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3013 mL	11.5067 mL	23.0134 mL	57.5334 mL
	5 mM	0.4603 mL	2.3013 mL	4.6027 mL	11.5067 mL
	10 mM	0.2301 mL	1.1507 mL	2.3013 mL	5.7533 mL
	15 mM	0.1534 mL	0.7671 mL	1.5342 mL	3.8356 mL
	20 mM	0.1151 mL	0.5753 mL	1.1507 mL	2.8767 mL
	25 mM	0.0921 mL	0.4603 mL	0.9205 mL	2.3013 mL
	30 mM	0.0767 mL	0.3836 mL	0.7671 mL	1.9178 mL
	40 mM	0.0575 mL	0.2877 mL	0.5753 mL	1.4383 mL
	50 mM	0.0460 mL	0.2301 mL	0.4603 mL	1.1507 mL
	60 mM	0.0384 mL	0.1918 mL	0.3836 mL	0.9589 mL
	80 mM	0.0288 mL	0.1438 mL	0.2877 mL	0.7192 mL
	100 mM	0.0230 mL	0.1151 mL	0.2301 mL	0.5753 mL

Keywords

Lexibulin

2 Cited Publications

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Lexibulin

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Heterocyclic Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) Lexibulin

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lexibulin

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Heterocyclic Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) Lexibulin

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lexibulin Related Classifications

HY-10498 Related Classifications