A RIPK1 inhibitor
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Ocadusertib

Item No. 46372

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-7-(3-hydroxy-3-methyl-1-butyn-1-yl)-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-5-carboxamide
CAS Number
2382811-41-6
Synonyms
  • LY3871801
  • R552
Molecular Formula
C25H25N5O4
Formula Weight
459.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Water (1:1): Sparingly soluble: 1-10 mg/mlMethanol: Sparingly soluble: 1-10 mg/ml
SMILES
OC(C)(C#CC(C=C1N2C)=CC=C1OC[C@H](NC(C3=NN=C(N3)CC4=CC=CC=C4)=O)C2=O)C
InChi Code
InChI=1S/C25H25N5O4/c1-25(2,33)12-11-17-9-10-20-19(13-17)30(3)24(32)18(15-34-20)26-23(31)22-27-21(28-29-22)14-16-7-5-4-6-8-16/h4-10,13,18,33H,14-15H2,1-3H3,(H,26,31)(H,27,28,29)/t18-/m0/s1
InChi Key
SQBZJKIINNRUFC-SFHVURJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $129

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    5 mg

    $613

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    $1,161

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    Product Description

    Ocadusertib is an inhibitor of receptor-interacting serine/threonine kinase 1 (RIPK1; IC50 = 0.038 µM).1 It is selective for RIPK1 over RIPK2 and RIPK3 (IC50s = >20 µM for both) and a panel of 105 kinases at 10 µM. Ocadusertib inhibits necroptosis induced by TNF and zVAD in U937 cells (EC50 = 3 nM) and apoptosis induced by TNF and (5Z)-7-oxozeaenol (Item No. 17459) in primary human T cells (EC50 = 0.4 nM). It inhibits hypothermia and decreases serum cytokine levels in a mouse model of sterile sepsis at 5 mg/kg. Ocadusertib also decreases disease severity in the Sharpincpdm mouse model of chronic proliferative dermatitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shaw, S.J., Taylor, V.C., Sims, J.T., et al. Early development of ocadusertib, a selective receptor-interacting serine/threonine-protein kinase 1 inhibitor. Clin. Transl. Sci. 19(3), (2026).