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

BMS-536924 

Cat. No.: HY-10262 Purity: 99.74%
Handling Instructions

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.

For research use only. We do not sell to patients.

BMS-536924 Chemical Structure

BMS-536924 Chemical Structure

CAS No. : 468740-43-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 92 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 624 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.
SMILES

O=C1C(C2=NC3=CC(N4CCOCC4)=CC(C)=C3N2)=C(C=CN1)NC[[email protected]@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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (104.18 mM; Need ultrasonic)

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
10 mM 0.2084 mL 1.0418 mL 2.0835 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

  • 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

*All of the co-solvents are provided by MCE.
References

Purity: 99.74%

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Keywords:

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

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BMS-536924
Cat. No.:
HY-10262
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