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Tyrosine Kinase/Adaptors IGF-1R BMS536924

BMS536924

Catalog No. T6419   CAS 468740-43-4
Synonyms: BMS 536924, BMS-536924, HY-10262, CS-0117, HY-10262, CS-0117, BMS-536924 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.

BMS536924, CAS 468740-43-4
Pack Size Availability Price/USD Quantity
5 mg In stock 80.00
10 mg In stock 134.00
50 mg In stock 566.00
1 mL * 10 mM (in DMSO) In stock 80.00
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Purity 99.19%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description 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 FAK : ic50 150nM ,   IGF-1R : ic50 100nM ,   Insulin Receptor : ic50 73nM ,   Lck : ic50 341nM ,   MEK : ic50 182nM
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)
Cell lines: TC32, HT1080/S, SK-LMS-1, H513 and CTR cells
Animal Research
Animal Model: TGBC-1TKB cells are subcutaneously injected into nude mice.
Synonyms BMS 536924 , BMS-536924 , HY-10262 , CS-0117 , HY-10262 , CS-0117 , BMS-536924 BMS 536924
Purity 99.19%
Molecular Weight 479.96
Formula C25H26ClN5O3
CAS No. 468740-43-4

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 89 mg/mL (185.4 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400/0.5% Tween80/5% propylene glycol: 30 mg/mL

Citations

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. 6. Huang F, et al, Cancer Res, 2009, 69(1), 161-170.

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