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SHP099

CAS No. : 1801747-42-1

產(chǎn)品活性：SHP099 is a potent, selective, orally available SHP2 inhibitor with an IC₅₀ of 70 nM.

研究領(lǐng)域：Protein Tyrosine Kinase/RTK  |  Metabolic Enzyme/Protease

作用靶點：SHP2  |  Phosphatase

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. 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.

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.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Metabolism/Protease Compound Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Orally Active Compound Library  |  Phosphatase Inhibitor Library  |  Human Metabolite Library  |  BN82002  |  Rubrofusarin 6-O-β-D-glucopyranoside  |  PF-04577806  |  RMC-3943  |  GNF362  |  MY10  |  D-erythro-Sphingosine  |  AS1949490  |  NTPDase-IN-1  |  SHP099 hydrochloride  |  Ertiprotafib  |  Trimyristin--d₁₅  |  SMAP-2  |  cyt-PTPε Inhibitor-1  |  Raphin1 acetate  |  Calyculin A  |  Endothall  |  Razuprotafib  |  Icerguastat  |  Methyl pseudolarate B  |  5-FAM-Alkyne  |  Calcium glycerophosphate  |  Trichomide A  |  PTP1B-IN-21  |  PFKFB3-IN-2  |  CD31  |  CCT007093  |  BVT948  |  L-690330 hydrate  |  SPI-112

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