SHP099

• CAT Number: I002342
• CAS Number: 1801747-42-1
• Molecular Formula: C16H19Cl2N5
• Molecular Weight: 352.3
• Purity: ≥95%
• Synonyms: 6-(4-amino-4-methyl-1-piperidinyl)-3-(2,3-dichlorophenyl)-2-pyrazinamine
• Target: target: SHP2
• Solubility: DMSO: ≤ 6.4 mg/mL (Need ultrasonic)
• Storage: -20°C
• InChIKey: YGUFCDOEKKVKJK-UHFFFAOYSA-N

SHP099 is a selective and orally bioavailable small-molecule SHP2 inhibitor with IC50 of 0.071 μM.target: SHP2IC 50: 0.071 μMIn vitro:SHP099 concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allostericmechanism. SHP099 suppresses RAS-ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells [1]In vivo: 1) SHP2 knockdown inhibits the growth of established KYSE520 xenograft tumours.2) plasma SHP099 concentration and xenograft p-ERK levels following a single oral administration of SHP099 (100 mg per kg)

Reference

[1]. Ying-Nan P et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases.