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詳細介紹 SHP099

產(chǎn)品活性：SHP099是有效，選擇性，有口服活性的 SHP2 抑制劑，IC50 值為70 nM。

研究領(lǐng)域：metabolic Enzyme/Protease

作用靶點：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 | Tacrolimus | SHP099 hydrochloride | Salubrinal | LB-100 | MSI-1436 lactate | Calyculin A | TPI-1 | Stibogluconate sodium | SF1670 | Sodium orthovanadate | β-Glycerol phosphate disodium salt pentahydrate | Microcystin-LR | NSC 663284 | GSK 2830371 | PTP1B-IN-2 | Rosiptor | TCS 401 | LTV-1 | Rilapladib | 3α-Aminocholestane | CPDA | Sal003 | BVT948 | PTP1B-IN-1 | RMC-4550 | (-)-p-Bromotetramisole oxalate | LMPTP INHIBITOR 1 dihydrochloride | Tetramisole hydrochloride

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