SHP099 free base

    • Catalog No.:MC1312
      • CasNo:
      • 1801747-42-1
      • MolecularFormula:
      • C16H19Cl2N5
      • Purity:
      • >99%
      • Target:
      • Discoidin Domain Receptor
      • IC50:
      • IC50: 70 nM (SHP2)[1]
      • In Vitro:
      • The X-ray co-crystal for SHP099 with SHP2 reveals a new interaction with the basic amine and the Phe113 backbone carbonyl. SHP099 shows inhibition of cell proliferation (KYSE-520 model) with an IC50 of 1.4 μM. SHP099 shows high solubility and high permeability with no apparent efflux in Caco-2 cells[1]. 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 allosteric mechanism. SHP099 suppresses RAS–ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells[2].
      • In Vivo:
      • After a single doses of 30 and 100 mg/kg (red and blue lines, respectively), dose-dependent exposure and modulation of the pharmacodynamic marker p-ERK is observed in the xenografts. A daily oral dose of 10 or 30 mg/kg yield 19% and 61% tumor growth inhibition, respectively. Tumor stasis is achieved at 100 mg/kg[1].
      • Fields:
      • SHP099 is a selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM.
      • Specificity:
      • Target: Discoidin Domain Receptor. Fields: SHP099 is a selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM.
      • Dilution:
      • IC50: 70 nM (SHP2)[1]
      • Concentration:
      • >99%
      • Storage Stability:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • Other Name:
      • SHP099,SHP 099,SHP-099
      • MolecularWeight(Da):
      • 352
      • References:
      • [1]. Garcia Fortanet J, et al. Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J Med Chem. 2016 Sep 8;59(17):7773-82. [2]. Chen YN,
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