SML2400
LW106
>97% (HPLC)
别名:
(4-Amino-1,2,5-oxadiazol-3-yl)(1,3-dihydro-2H-isoindol-2-yl)-methanone oxime, (E)-(4-Amino-1,2,5-oxadiazol-3-yl)(isoindolin-2-yl)methanone oxime
SMILES string
O/N=C(C1=NON=C1N)/N2CC3=CC=CC=C3C2
assay
>97% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Indoleamine 2,3-dioxygenase 1 (IDO; IDO1) inhibitor with better in vivo antitumor efficacy than Epacadostat (INCB024360).
LW106 is an indoleamine 2,3-dioxygenase 1 (IDO; IDO1) inhibitor (IC50 = 13 nM) that effectively inhibits kynurenine production upon cellular IDO1 upregulation by IFNγ induction (50 ng/mL, 48 h) in HeLa cultures (IC50 = 1.57 μM) and prevents the antiproliferation activity of IDO1-positive DCs against co-cultured CD8+ T-cells (proliferation suppression = 67% with vehicle vs. 33% with 20 μM LW106). LW106 exhibits antitumor activity only in immunocompetent, but not athymic or IDO1-/-, mice, displaying better in vivo efficacy than Epacadostat (Lewis lung carcinoma/B16-F10 tumor suppression = 68%/65% with LW106 vs. 51%/50% with Epacadostat; 80 mg/kg/day i.p.).
存储类别
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Rong Fu et al.
British journal of pharmacology, 175(14), 3034-3049 (2018-05-04)
Indoleamine 2,3-dioxygenase 1 (IDO1) is emerging as an important new therapeutic target for treatment of malignant tumours characterized by dysregulated tryptophan metabolism. However, the antitumour efficacy of existing small-molecule inhibitors of IDO1 is still unsatisfactory and the underlying mechanism remains
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