ORY-1001 trans and cis isomers

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ORY-1001 (RG-6016) 是一种高效、选择性的赖氨酸特异性去甲基酶 KDM1A (LSD1) 抑制剂，IC50 为 18 nM。

ORY-1001 (RG-6016) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases; exhibits low nanomolar cellular activity (EC50 < 1 nM) in the THP1 differentiation assay and induces the CD11b marker within 6 hr of treatment in FACS based differentiation assay in THP1 cell line; induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML; exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models.Blood Cancer Phase 2 Clinical.

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RG 6016 | RG6016 | RG-6016 | ORY1001 | ORY 1001

Chromatin/Epigenetic

Histone Demethylase

LSD1/KDM1A

Cancer

Blood cancer

1431326-61-2

303.2704

C15H24Cl2N2

>98% (HPLC)

DMSO: < 6.8 mg/mL

NC1CCC(N[C@@H]2C[C@H]2C3=CC=CC=C3)CC1.Cl.Cl

1,4-Cyclohexanediamine, N1-[(1R,2S)-2-phenylcyclopropyl]-, hydrochloride (1:2), rel-

(-20℃)

With Ice Pack

≥ 2 years