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Darovasertib

Chemical Structure : Darovasertib

CAS No.: 1874276-76-2

Darovasertib (NVP-LXS196, LXS196, IDE196)

Catalog No.: PC-38356Not For Human Use, Lab Use Only.

Darovasertib (NVP-LXS196, LXS 196, IDE 196) is a potent, selectve, oral pan- protein kinase C (PKC) inhibitor with IC50 of 3 nM and 0.6 nM for PKCα and PKCθ, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Darovasertib (NVP-LXS196, LXS 196, IDE 196) is a potent, selectve, oral pan- protein kinase C (PKC) inhibitor with IC50 of 3 nM and 0.6 nM for PKCα and PKCθ, respectively.
Darovasertib (NVP-LXS196, LXS 196, IDE 196) demonstrates high potency toward classical PKC isoforms (IC50s=2.9-1.9 nM).
Darovasertib (NVP-LXS196, LXS 196, IDE 196) shows comparable cellular potency (IC50=170 nM) versus AEB071 in the 92.1 cellular proliferation assays.
Darovasertib (NVP-LXS196, LXS 196, IDE 196) demonstrates antitumor efficacy and tolerability in the 92.1 tumor xenograft model in mice.

Physicochemical Properties

M.Wt 472.47
Formula C22H23F3N8O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide

References

1. Ellen Kapiteijn, et al. Cancer Res (2019) 79 (13_Supplement): CT068.

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