SGI-1776 [1025065-69-3]

Catalog number: HY-13287_5mg
Brand: MedChem Express
Packing: 5 mg
Other sizes: Other sizes available
Price: € 144.00
Expected delivery time: 10 days

Product specifications for - SGI-1776 [1025065-69-3]

Product group: Chemicals
Category: Other
CAS No.: 1025065-69-3
Purity: >98%
Molecular Formula: C20H22F3N5O
Molecular weight: 405.42
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. IC50 value: 7 nM [1] Target: Pim1 in vitro: In addition to Pim, SGI-1776 also potently targets FLT3 (IC50 = 44nM). Treatment of AML cells with SGI-1776 results in a concentration-dependent induction of apoptosis. Importantly, SGI-1776 is also cytotoxic in AML primary cells, irrespective of FLT3 mutation status and results in Mcl-1 protein decline [1]. Treatment of CLL cells with SGI-1776 results in a concentration-dependent induction of apoptosis. SGI-1776 induces apoptosis in CLL and that the mechanism involves Mcl-1 reduction. Apoptosis induction coupled with the inhibition of RNA synthesis is observed in CLL cells treated with SGI-1776 [2]. SGI-1776 exhibites cytotoxic activity in vitro with a median relative IC50 of 3.1 mM. SGI-1776 induces tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induces complete responses of subcutaneous MV4,11 [3]. in vivo: Consistent with cell line data, xenograft model studies with mice bearing MV-4-11 tumors shows efficacy with SGI-1776. [1] SGI-1776 has shown preclinical activity against leukemia and solid tumor cell line models with IC50 values of 0.005-11.68 mM. SGI-1776 induces significant differences in EFS distribution in vivo in 9 of 31 solid tumor xenografts and in 1 of 8 of the evaluable ALL xenografts [3].
Safety information: 
Additional information: 
Synonyms: HY-13287
Science. 2017 Dec 1;358(6367):eaan4368. Read more
Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. Read more
J Med Chem. 2021 Oct 21. Read more
eNeuro. 2019 Aug 22;6(4):ENEURO.0003-19.2019. Read more
Cell Death Dis. 2018 Feb 22;9(3):307. Read more
Patent. US20180263995A1. Read more