Crenigacestat


CAS No. : 1421438-81-4

(Synonyms: LY3039478)

1421438-81-4
Price and Availability of CAS No. : 1421438-81-4
Size Price Stock
1mg $71 In-stock
5mg $150 In-stock
10mg $250 In-stock
25mg $450 In-stock
50mg $750 In-stock
100mg $1250 In-stock
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Cat. No. : HY-12449
M.Wt: 464.44
Formula: C22H23F3N4O4
Purity: >98 %
Solubility: DMSO : ≥ 34 mg/mL
Introduction of 1421438-81-4 :

Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested[1][2][3][4]. In Vitro: Crenigacestat (100 nM) exhibits anti-cancer activity in K07074 cells (a primary mouse liver tumor cell line)[2].
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[3]. In Vivo: Crenigacestat (8 mg/kg, oral gavage three times a week) resulted in significantly increases survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC[3].

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