IadademSTAT dihydrochloride 是一种不可逆的选择性赖氨酸特异性脱甲基酶 1A (KDM1A/LSD1) 抑制剂,用于治疗急性白血病。
产品描述
ORY-1001, a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.
体外活性
ORY-1001 is a highly potent and selective KDM1A inhibitor that induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML.
体内活性
ORY-1001 exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of an AML xenograft model, and extends survival in a mouse PDX (patient-derived xenograft) model of T cell acute leukemia.?Surrogate pharmacodynamic biomarkers developed based on expression changes in leukemia cell lines were translated to samples from patients treated with ORY-1001.?ORY-1001 is a selective KDM1A inhibitor in clinical trials and is currently being evaluated in patients with leukemia and solid tumors.
Cas No.
1431303-72-8
分子式
C15H24Cl2N2
分子量
303.27
别名
ORY-1001(trans)
储存和溶解度
DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years