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ICG-001

Cat. No. M2008
ICG-001 Structure
Synonym:

PRI-724 isomer

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 56  USD56 In stock
5mg USD 75  USD75 In stock
10mg USD 109  USD109 In stock
50mg USD 407  USD407 In stock
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Quality Control
Biological Activity

ICG-001 selectively inhibits β-catenin/CBP interaction. ICG-001 exhibits growth inhibitory effects in colon carcinoma cell lines (SW480 and HCT-116 cells). ICG-001 also displays efficacy in Min mouse and nude mouse SW620 xenograft models. ICG-001 selectively induces apoptosis in transformed cells but not in normal colon cells, reduces in vitro growth of colon carcinoma cells, and is efficacious in the Min mouse and nude mouse xenograft models of colon cancer. ICG-001 (5 mg/kg per day) significantly inhibits beta-catenin signaling and attenuates bleomycin-induced lung fibrosis in mice, while concurrently preserving the epithelium. Administration of ICG-001 concurrent with bleomycin prevents fibrosis, and late administration is able to reverse established fibrosis and significantly improve survival.

Product Citations
Customer Product Validations & Biological Datas
Source Oncogene (2014). Figure 1. ICG-001 was purchased from AbMole BioSciences (Kowloon, Hong Kong, China)
Method microscopy images
Cell Lines IEC-6 caMEK
Concentrations 7.5 µ M
Incubation Time 36 h
Results "The caMEK-transformed cells showed a partial reversion to an epithelial morphology after treatment of caMEK-transformed cells with ICG-001, a small-molecule antagonist of β-catenin/ TCF-mediated transcription."
Protocol
Cell Experiment
Cell lines NCI-H929, U266, MM1S, and RPMI-8226
Preparation method Cells were treated with various concentrations of ICG-001 for 24 hours. 3-[4, 5-Dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide (MTT) dye (Sigma) was added for the last 4 hours of incubation. Insoluble formazan complexes were pelleted and solubilized with DMSO, and absorbance was measured at 540 nm using a Benchmark Plus microplate spectrophotometer (Bio-Rad, Hercules, CA). The IC50 values were calculated using CalcuSyn software (Biosoft, Cambridge, UK). Each experimental condition was done in triplicate and repeated at least once.
Concentrations 0-50 µ M
Incubation time 24 h
Animal Experiment
Animal models MM tumors were established in SCID-beige mice by subcutaneous inoculation of 1x107 MM RPMI-8226 cells in the right flank
Formulation Solubilized in DMSO and diluted with PBS containing 10% dimethylacetamide (Sigma-Aldrich) and 6% Solutol (Sigma-Aldrich).
Dosages 100 mg/kg ICG-001 twice a day
Administration administered intraperitoneally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 548.63
Formula C33H32N4O4
CAS Number 780757-88-2
Purity 100.00%
Solubility DMSO ≥ 50 mg/mL
Storage at -20°C
References

[1] Zhou B, et al. J Biol Chem. Interactions between β-catenin and transforming growth factor-β signaling pathways mediate epithelial-mesenchymal transition and are dependent on the transcriptional co-activator cAMP-response element-binding protein (CREB)-binding protein (CBP).

[2] Henderson WR Jr, et al. Proc Natl Acad Sci U S A. Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis.

[3] Emami KH, et al. Proc Natl Acad Sci U S A. A small molecule inhibitor of beta-catenin/CREB-binding protein transcription.

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  Catalog
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Keywords: ICG-001, PRI-724 isomer supplier, Wnt/beta-catenin, inhibitors

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