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LY3039478

Cat. No. M2827

All AbMole products are for research use only, cannot be used for human consumption.

LY3039478 Structure
Synonym:

Crenigacestat

Size Price Availability Quantity
2mg USD 96  USD96 In stock
5mg USD 136  USD136 In stock
10mg USD 220  USD220 In stock
25mg USD 440  USD440 In stock
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Quality Control & Documentation
Biological Activity

LY3039478 (Crenigacestat) is a novel and orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested. Crenigacestat (LY3039478) decreases expression of Myc and cyclin A1 (part of the NOTCH-driven proliferative signature) in murine and human model systems. Crenigacestat (LY3039478) treatment also leads to G0/G1 cell cycle arrest in CCRCC cells.

Customer Product Validations & Biological Datas
Source J Biol Chem (2017). Figure 6. LY3039478
Method qRT-PCR
Cell Lines CCRCC cell lines
Concentrations 1 μM
Incubation Time -
Results Treatment with a secretase inhibitor that is being tested in clinical trials, LY3039478, significantly inhibited the growth of 2 CCRCC cell lines in a concentrationdependent manner
Chemical Information
Molecular Weight 464.44
Formula C22H23F3N4O4
CAS Number 1421438-81-4
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Analia Azaro, et al. A phase 1b study of the Notch inhibitor crenigacestat (LY3039478) in combination with other anticancer target agents (taladegib, LY3023414, or abemaciclib) in patients with advanced or metastatic solid tumors

[2] Gautam Borthakur, et al. Phase 1 study to evaluate Crenigacestat (LY3039478) in combination with dexamethasone in patients with T-cell acute lymphoblastic leukemia and lymphoma

[3] Margot J Pont, et al. γ-Secretase inhibition increases efficacy of BCMA-specific chimeric antigen receptor T cells in multiple myeloma

[4] Olivier Mir, et al. Notch pathway inhibition with LY3039478 in soft tissue sarcoma and gastrointestinal stromal tumours

[5] C Massard, et al. First-in-human study of LY3039478, an oral Notch signaling inhibitor in advanced or metastatic cancer

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Keywords: LY3039478, Crenigacestat supplier, Gamma-secretase/Beta-secretase, inhibitors, activators

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