2. Protein Tyrosine Kinase/RTK Apoptosis
  3. IGF-1R Insulin Receptor Apoptosis
  4. BMS-536924

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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BMS-536924 Chemical Structure

BMS-536924 Chemical Structure

CAS No. : 468740-43-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 97 In-stock
Solution
10 mM * 1 mL in DMSO USD 97 In-stock
Solid
1 mg USD 43 In-stock
5 mg USD 92 In-stock
10 mg USD 158 In-stock
50 mg USD 686 In-stock
100 mg USD 800 In-stock
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Based on 3 publication(s) in Google Scholar

BMS-536924 Related Antibodies

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  • Purity & Documentation

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Description

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[1][2].

IC50 & Target

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

BMS-536924 Related Antibodies

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.
Molecular Weight

479.96

Formula

C25H26ClN5O3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0835 mL 10.4175 mL 20.8351 mL
5 mM 0.4167 mL 2.0835 mL 4.1670 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.83%

COA (256 KB) LCMS (267 KB) OR (62 KB)

Handling Instructions (2659 KB)
References

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
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BMS-536924 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:

BMS-536924468740-43-4BMS536924BMS 536924IGF-1RInsulin ReceptorApoptosisInsulin-like growth factor-1 receptorOrallyinsulin-likegrowthfactorbreastcancer,Inhibitorinhibitorinhibit

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