SHP244

SHP244 is a conformational inhibitor targeting the "latch allosteric site" (site 2) of the SHP2 protein with an IC50 value for SHP2WT of 60 μM. SHP244 has no significant effect on the level of p-ERK alone. SHP244 combined with RMC-4550 (HY-116009) ("tunnel site" site 1 inhibitor) can reduce p-ERK and inhibit the rebound of p-ERK, thereby reducing drug resistance. SHP244 can be used to study drug resistance in FGFR-driven cancers[1].

Product Specifications

CAS Number

[902891-37-6]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

SHP2

Related Pathways

Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

O=C1C2=C(N3C(C4=C(O)C(OC)=CC=C4)=NN=C3N1CC5=C(Cl)C=CC=C5)C=CC=C2

Molecular Formula

C23H17ClN4O3

Molecular Weight

432.86

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P362+P364-P405-P501

References & Citations

[1]Lu H, et al. Resistance to allosteric SHP2 inhibition in FGFR-driven cancers through rapid feedback activation of FGFR. Oncotarget. 2020 Jan 21;11 (3) :265-281.|[2]Song Y, et al. Crystallographic landscape of SHP2 provides molecular insights for SHP2 targeted drug discovery. Medicinal Research Reviews. 2022 Sep;42 (5) :1781-821.