BMS-536924
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.83%
- CAS No.: 468740-43-4
- Formule: C25H26ClN5O3
- Masse moléculaire:479.96
-
Stockage:Powder -20°C, 3 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Differentiation Inducing Compound Library
HY-L038
-
Orally Active Compound Library
HY-L061
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Angiogenesis-Related Compound Library
HY-L088
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Metabolic Enzyme Compound Library
HY-L146
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cytokine Inhibitors Library
HY-L161
-
Cell Death Library
HY-L162
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
Anti-Aging Compound Library Mini
HY-L034M
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) BMS-536924
More
Activité biologique
|
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] |
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 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 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.
-
Cell Line:CD8-IGF-IR-MCF10A acini
-
Concentration:1 μM
-
Incubation Time:For 4 days
-
Result:Resulted in a dramatic induction of apoptosis.
-
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.
-
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.
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 No. 468740-43-4
-
Appearance Solid
-
Masse moléculaire 479.96
-
Formule 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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years In solvent -80°C 1 year -20°C 6 months
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
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
2025 Apr 14:S0363-5023(25)00132-7. PMID: 40232216 -
Gen Comp Endocrinol
2019 Sep 15:281:83-90. PMID: 31170402
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
-
Fiche technique (285 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
BMS-536924 Related Classifications
HY-10262 Related Classifications
Powered by Bioz