902891-37-6
Chemical Structure
SHP244
- CAS No.: 902891-37-6
- Formula:C23H17ClN4O3
- Molecular Weight:432.86
IUPAC Name: 4-(2-chlorobenzyl)-1-(2-hydroxy-3-methoxyphenyl)-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one
InChIKey: MUHNHVCFKYIXPU-UHFFFAOYSA-N
SMILES: O=C1C2=C(N3C(C4=C(O)C(OC)=CC=C4)=NN=C3N1CC5=C(Cl)C=CC=C5)C=CC=C2
Biological Activity: 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].
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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. | |||||||||||||||||||||
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Keywords
