Art. -Nr.: HY-10262

BMS-536924

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC₅₀s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.

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Reinheit: 99.83%
CAS. Nr.: 468740-43-4
Formel: C₂₅H₂₆ClN₅O₃
Molecular Weight:479.96

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 1 year , -20°C, 6 months

BMS-536924 Chemical Structure

CAS. Nr.: 468740-43-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 100 nM (IGF-1R) and 73 nM (IR)^[1]^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	212 nM Compound: 20, BMS-536924	Cytotoxicity against human COLO205 cells Cytotoxicity against human COLO205 cells	[PMID: 19610618]
COLO 205	IC₅₀	212 nM Compound: 3, BMS-536924	In vitro inhibitory concentration against COLO 205 (colon) cell line with ATP concentration at 1/2Km In vitro inhibitory concentration against COLO 205 (colon) cell line with ATP concentration at 1/2Km	[PMID: 16134929]
LS174T	IC₅₀	2.05 μM Compound: BMS-536924	Antiproliferative activity against human LS 174T cells after 48 hrs by MTT assay Antiproliferative activity against human LS 174T cells after 48 hrs by MTT assay	[PMID: 25648298]
MCF7	IC₅₀	1.748 μM Compound: BMS-536924	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 25648298]
MCF7	IC₅₀	460 nM Compound: 20, BMS-536924	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 19610618]
MCF7	IC₅₀	460 nM Compound: 3, BMS-536924	In vitro inhibitory concentration against MCF-7(breast) cell line with ATP concentration at 1/2Km In vitro inhibitory concentration against MCF-7(breast) cell line with ATP concentration at 1/2Km	[PMID: 16134929]
RD	IC₅₀	202 nM Compound: 3, BMS-536924	In vitro inhibitory concentration against RD1 (rhabdomyosarcoma) cell line with ATP concentration at 1/2Km In vitro inhibitory concentration against RD1 (rhabdomyosarcoma) cell line with ATP concentration at 1/2Km	[PMID: 16134929]
SGC-7901	IC₅₀	2.893 μM Compound: BMS-536924	Antiproliferative activity against human SGC7901 cells after 48 hrs by MTT assay Antiproliferative activity against human SGC7901 cells after 48 hrs by MTT assay	[PMID: 25648298]
SMMC-7721	IC₅₀	2.555 μM Compound: BMS-536924	Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay	[PMID: 25648298]

In Vitro

BMS-536924 inhibits FAK and Lck with IC₅₀s of 150 nM and 341 nM, respectively^[1].
BMS-536924 (1 μM; every four days for 12 days) blocks pBabe-MCF10A and CD8-IGF-IR-MCF10A acinar proliferation^[2].
BMS-536924 (0.01-1 μM; 24 hours) inhibits growth of CD8-IGF-IR-MCF10A cells and has an IC₅₀ of 0.48 μM^[2].
BMS-536924 (1 μM; for 4 days) induces apoptosis in CD8-IGF-IR-MCF10A acini^[2].
BMS-536924 (0.1-1 μM; for 24 hours) decreases in S-phase cells and causes a G0/G1 block^[2].
BMS-536924 (1 μM; 10 min, 1, 8, 24, 48 hours) inhibits IGF-IR signaling in pBabe-MCF10A cells and inhibits phosphorylation of CD8-IGF-IR. BMS-536924 time-dependently inhibits AKT phosphorylation^[2].

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

Cell Proliferation Assay^[2]

Cell Line:

pBabe-MCF10A and CD8-IGF-IR-MCF10A acini
Concentration:

1 μM
Incubation Time:

Every four days for 12 days
Result:

Blocked acinar proliferation.

Cell Viability Assay^[2]

Cell Line:

CD8-IGF-IR-MCF10A cells
Concentration:

0.01, 0.1, 1 μM
Incubation Time:

24 hours
Result:

Has an IC50 of 0.48 μM.

Apoptosis Analysis^[2]

Cell Line:

CD8-IGF-IR-MCF10A acini
Concentration:

1 μM
Incubation Time:

For 4 days
Result:

Resulted in a dramatic induction of apoptosis.

Cell Cycle Analysis^[2]

Cell Line:

CD8-IGF-IR-MCF10A cells and pBabe-MCF10A control cells
Concentration:

0.1, 0.5, 1 μM
Incubation Time:

For 24 hours
Result:

Decreased in S-phase cells and caused a G0/G1 block.

Western Blot Analysis^[2]

Cell Line:

CD8-IGF-IR-MCF10A cells
Concentration:

1 μM
Incubation Time:

10 min, 1, 8, 24, 48 hours
Result:

Caused maximal inhibition of phosphorylated IGF-IR at 10 min and retained its ability to inhibit IGF-IR phosphorylation for up to 48 hours.

In Vivo

BMS-536924 (100 mg/kg; gavage; daily; for 35 days) causes regression of xenografts in vivo and an average reduction of 76% tumor volume after 2 weeks^[2].

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

Animal Model:

Athymic nude mice with CD8-IGF-IRMCF10A cells^[2]
Dosage:

100 mg/kg
Administration:

Gavage; daily; for 35 days
Result:

Caused an average reduction of 76% tumor volume after 2 weeks.

Chemical Information

CAS. Nr. 468740-43-4
Appearance Solid
Molecular Weight 479.96
Formel C₂₅H₂₆ClN₅O₃
Color Light yellow to yellow
SMILES

O=C1C(C2=NC3=CC(N4CCOCC4)=CC(C)=C3N2)=C(C=CN1)NC[C@@H](O)C5=CC=CC(Cl)=C5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (5)

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Journal Impact Factor

Nat Commun

CNK2 promotes cancer cell motility by mediating ARF6 activation downstream of AXL signalling. [Abstract]

2023 Jun 15;14(1):3560. PMID: 37322019
Cell Discov

Reprogramming of palmitic acid induced by dephosphorylation of ACOX1 promotes β-catenin palmitoylation to drive colorectal cancer progression. [Abstract]

2023 Mar 7;9(1):26. PMID: 36878899
BMC Med

IGF1-mediated mesenchymal-endothelial transition as a potential regulatory target in calcific aortic valve disease. [Abstract]

2025 Nov 3;23(1):600. PMID: 41184837
J Hand Surg Am

Transforming Myofibroblasts Into Lipid-Filled Cells to Treat Dupuytren Disease. [Abstract]

2025 Apr 14:S0363-5023(25)00132-7. PMID: 40232216
Gen Comp Endocrinol

Insulin-like growth factor binding proteins inhibit oocyte maturation of zebrafish. [Abstract]

2019 Sep 15:281:83-90. PMID: 31170402

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 10 mg/mL (20.84 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.0835 mL

10.4175 mL

20.8351 mL

5 mM

0.4167 mL

2.0835 mL

4.1670 mL

10 mM

0.2084 mL

1.0418 mL

2.0835 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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: ≥ 3.75 mg/mL (7.81 mM); Clear solution

This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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 (5.21 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.25 mg/mL (4.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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 (285 KB)
SDS (252 KB)
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- Swedish - SV (252 KB)
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- Portuguese - PT (252 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]. Wittman M, et al. Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J Med Chem. 2005 Sep 8;48(18):5639-43. [Content Brief]

[2]. Litzenburger BC, et al. BMS-536924 reverses IGF-IR-induced transformation of mammary epithelial cells and causes growth inhibition and polarization of MCF7 cells. Clin Cancer Res. 2009 Jan 1;15(1):226-37. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0835 mL	10.4175 mL	20.8351 mL	52.0877 mL
	5 mM	0.4167 mL	2.0835 mL	4.1670 mL	10.4175 mL
	10 mM	0.2084 mL	1.0418 mL	2.0835 mL	5.2088 mL
	15 mM	0.1389 mL	0.6945 mL	1.3890 mL	3.4725 mL
	20 mM	0.1042 mL	0.5209 mL	1.0418 mL	2.6044 mL

Keywords

BMS-536924

5 Cited Publications

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BMS-536924

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) BMS-536924

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-536924

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) BMS-536924

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-536924 Related Classifications

HY-10262 Related Classifications