| Identification | Back Directory | [Name]
Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-, (αR)- | [CAS]
2170140-50-6 | [Synonyms]
(R)-GSK-3685032
Benzeneacetamide, α-[[6-(4-amino-1-piperidinyl)-3,5-dicyano-4-ethyl-2-pyridinyl]thio]-, (αR)- | [Molecular Formula]
C22H24N6OS | [MOL File]
2170140-50-6.mol | [Molecular Weight]
420.54 |
| Chemical Properties | Back Directory | [Boiling point ]
669.4±55.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, away from moisture and light | [solubility ]
DMSO : 60 mg/mL (142.68 mM; Need ultrasonic) | [form ]
Solid | [pka]
14.65±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition[1][2]. | [References]
[1]. Adams, Nicholas David, et al. Substituted pyridines as inhibitors of DNMT1 and their preparation. WO2017216727A1. [2]. Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nat Cancer. 2021;2(10):1002-1017. |
|
|