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PF-07284892

Chemical Structure : PF-07284892

CAS No.: 2498597-94-5

PF-07284892 (PF 07284892, ARRY-558, ARRY558)

Catalog No.: PC-72611Not For Human Use, Lab Use Only.

PF-07284892 (ARRY-558) is a potent, selective allosteric SHP2 inhibitor with IC50 of 21 nM, has 1,000-fold selectivity for SHP2 over 21 other phosphatases, including the closely related SHP1.

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Purity & Documentation Purity: 99.4% (HPLC) Select Batch:

Biological Activity

PF-07284892 (ARRY-558) is a potent, selective allosteric SHP2 inhibitor with IC50 of 21 nM, has 1,000-fold selectivity for SHP2 over 21 other phosphatases, including the closely related SHP1.
PF-07284892 potently inhibits phosphorylated ERK (pERK) with low nanomolar IC50 values.
PF-07284892 shows improved brain penetration compared with other SHP2 inhibitors.
PF-07284892 overcomes bypass-signaling-mediated resistance when combined with inhibitors of various oncogenic drivers.

Physicochemical Properties

M.Wt 439.96
Formula C21H22ClN7S
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

(S)-1'-(6-((3-amino-2-chlorophenyl)thio)-1,2,4-triazin-3-yl)-1,3-dihydrospiro[indene-2,4'-piperidin]-1-amine

References

1. Drilon A, et al. Cancer Discov. 2023 Aug 4;13(8):1789-1801.

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