Oditrasertib free base · Synonyms: DNL788 | SAR443820
Oditrasertib is an orally active, BBB-penatrable and selective reversible inhibitor of RIPK1.
For research use only. Not for human or veterinary use.
Target
RIP kinase
Purity >98%
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Oditrasertib structure
CAS No.: 2252271-93-3
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Description
Oditrasertib (SAR443820) is an orally active, BBB-penatrable and selective reversible inhibitor of RIPK1. Oditrasertib can be used in the research of chronic inflammatory central nervous system diseases, such as amyotrophic lateral sclerosis and multiple sclerosis.
Biological activity
In Vitro Oditrasertib has a 50% inhibitory concentration of 3.16 nM in human PBMCs and 1.6 nM in iPSC-derived microglia.
Specifications
- MW (average)
- 295.2846
- Formula
- C14H15F2N3O2
- CAS No.
- 2252271-93-3
- Physical state
- Solid
- Color
- white to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder 4℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO
Documents
References
[1]. Fidalgo JDV, et al. Preparation of substituted oxazepines and related compounds as RIPK1 inhibitors and uses thereof. WO2018213632A1. 2018-11-22.
[2]. Hincelin-Mery A, et al. Safety, pharmacokinetics, and target engagement of a brain penetrant RIPK1 inhibitor, SAR443820 (DNL788), in healthy adult participants. Clin Transl Sci. 2024 Jan;17(1):e13690.
[3]. Montalban X, et al. Effect of RIPK1 inhibitor, SAR443820, on serum neurofilament light levels in patients with multiple sclerosis: a phase 2 trial design (P6-3.011)[J]. Neurology, 2023, 100(17_supplement_2): 2178.