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BMS-536924

Catalog No. T6419 CAS 468740-43-4

Synonyms: HY-10262, BMS 536924, CS-0117

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.

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BMS-536924, CAS 468740-43-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
5 mg	In stock	$ 74.00
10 mg	In stock	$ 129.00
25 mg	In stock	$ 258.00
50 mg	In stock	$ 495.00
100 mg	In stock	$ 663.00
1 mL * 10 mM (in DMSO)	In stock	$ 78.00

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Purity: 99.19%

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Description	BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.
Targets&IC50	Insulin receptor:73 nM, IGF-1R:100 nM
In vitro	BMS-536924 also inhibits FAK and Lck with IC50 of 150 nM and 341 nM, respectively. BMS-536924 inhibits cellular proliferation and disrupts Akt and MAPK phosphorylation. [1] BMS-536924 inhibits IGF-I-stimulated IGF-1R signaling in MCF10A cells and blocks constitutive IGF-1R activity in CD8-IGF-1R-MCF10A. Preincubation of MCF10A cells with 1 μM BMS-536924 completely blocks the ability of IGF-I to stimulate IGF-1R phosphorylation. IGF-I stimulation results in increased phosphorylation of ERK1/2, GSK3β, and Akt. BMS-536924 inhibits this ligand-induced phosphorylation. Treatment of the CD8-IGF-1R-MCF10A cells with BMS-536924 results in a dose-dependent inhibition of phosphorylation with partial inhibition at 0.01 μM and 0.1 μM, but complete receptor inhibition at a concentration of 1 μM. Maximal inhibition of phosphorylated IGF-1R is observed as early as 10 minutes following incubation. BMS-536924 retains its ability to inhibit IGF-1R phosphorylation for up to 48 hours. Addition of BMS-536924 time-dependently inhibits Akt phosphorylation starting at 1 hour. By 48 hours, Akt activation is completely blocked. [2] Treatment with BMS-536924 shows antiproliferation activity in a panel of cancer cell lines including TC32, HT1080/S, SK-LMS-1, H513 and CTR cells. pIGF-1R/pIR is activated upon IGF-I/insulin stimulation and the activation is inhibited by BMS-536924 at similar potencies in Rh41 and Rh36 cell lines. The expression of programmed cell death 4 (PDCD4), cleavage of poly(ADP-ribose) polymerase (PARP) and caspase-3 are up-regulated in Rh41 cells treated with BMS-536924. [3]
In vivo	Oral administration of BMS-536924 at 100-300 mpk strongly inhibits IGR-1R Sal tumor model. Efficacy is also observed in the nonengineered Colo205 human colon carcinoma mode. Oral administration of 3 on a once a day schedule (100-300 mpk) or a twice a day schedule (50, 100 mpk) demonstrates antitumor activity in this tumor model. Oral glucose tolerance test (OGTT) shows 100 mpk (b.i.d.) causes a significant elevation in glucose levels after glucose challenge. The pharmacokinetic parameters of BMS-536924, administered orally in poly(ethylene glycol) 400 and water (80:20 v/v), are determined in mouse, rat, dog, and monkey. Good bioavailability is evident in all species. Significant nonlinear pharmacokinetics is observed in rodents at increasing p.o. dose. [1] BMS-536924 reduces the tumor xenografts volume of CD8-IGF-1R-MCF10A cells after two weeks' treatment (100 mg/kg) to 76%. [2] Oral administration of 70 mg/kg BMS-536924 significantly inhibits tumor growth (TGBC-1TKB cells) inoculated in nude mice. BMS-536924 up regulates apoptosis in xenografts tumors. The treatment doesn't have adverse effects on the body weight of mice or the glucose levels at the time of death, suggesting tolerable toxicity. [4]
Kinase Assay	IGF-I Pathway Activity: 1 × 106 pBabe-MCF10A cells are seeded onto 60-mm dishes. After 24 hours, the medium is changed to serum-free medium and incubated overnight at 37 °C for 24 hours. Cells are then pre-incubated with or without 1 uM BMS-536924 for 1 hour in serum free medium followed by stimulation with IGF-I (50 ng/mL) for 10 minutes. Cell monolayers are washed twice with PBS and harvested for immunoblot analysi
Cell Research	Cell proliferation is evaluated by [3H]thymidine incorporation after exposure to BMS-536924 for 72 hours. Cells are plated at an optimized density in 96-well plates, incubated overnight at 37 °C, and then exposed to a serial dilution of the drug. After a 72-hours incubation, cells are pulsed with 4 μCi/mL [3H]thymidine for 3 hours, trypsinized, harvested onto UniFilter-96 GF/B plates; scintillation is measured on a TopCount NXT. Results are expressed as an IC50. The mean IC50 and SD from multiple tests for each cell line are calculated. (Only for Reference)

Synonyms	HY-10262, BMS 536924, CS-0117
Molecular Weight	479.96
Formula	C25H26ClN5O3
CAS No.	468740-43-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 89 mg/mL (185.4 mM)

References and Literature

1. Wittman M, et al. J Med Chem, 2005, 48(18), 5639-5643 2. Litzenburger BC, et al. Clin Cancer Res, 2009, 15(1), 226-237 3. Huang F, et al. Cancer Res, 2009, 69(1), 161-170 4. Hirokazu Ohashi, et al. Cancer Sci, 2012, 103(2), 252-261 5. Haluska P, et al, Mol Cancer THer, 2008, 7(9), 2589-2598.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Kinase Inhibitor Library Orally Active Compound Library Apoptosis Compound Library MAPK Inhibitor Library Anti-Ovarian Cancer Compound Library Glycometabolism Compound Library Preclinical Compound Library

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Related compounds with same targets

Ethylene dimethanesulfonate CSN5i-3 Urolithin A DPN D4476 Penicillic acid CP 461 LDC000067

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Keywords

BMS-536924 468740-43-4 Angiogenesis Apoptosis Cytoskeletal Signaling MAPK Tyrosine Kinase/Adaptors Src IGF-1R MEK FAK HY10262 HY-10262 inhibit CS 0117 Insulin Receptor Inhibitor insulin-like BMS 536924 cancer factor breast CS-0117 HY 10262 BMS536924 growth CS0117 Orally inhibitor

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