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- 技术资料
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Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：1-2天
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10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥880.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥800.0 |
| 规格： | 10 mg | 产品价格： | ￥1450.0 |
| 规格： | 25 mg | 产品价格： | ￥2360.0 |
| 规格： | 50 mg | 产品价格： | ￥3580.0 |
| 规格： | 100 mg | 产品价格： | ￥5000.0 |
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SHP099
CAS No. : 1801747-42-1
MCE 国际站：SHP099
产品活性：SHP099是有效，选择性，有口服活性的 SHP2 抑制剂，IC50 值为70 nM。
研究领域：Protein Tyrosine Kinase/RTK | Metabolic Enzyme/Protease
作用靶点：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 dose 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.
相关产品：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 | Highly Selective Inhibitors Library | Cyclosporin A | Tacrolimus | Calyculin A | β-Glycerophosphate disodium salt pentahydrate | Salubrinal | Okadaic acid | Ebselen | Batoprotafib | Ellagic acid | L-Ascorbic acid 2-phosphate trisodium | Sodium orthovanadate | Suramin sodium salt | RMC-4550 | TPI-1 | Vociprotafib | SHP099 monohydrochloride | Osunprotafib | DT-061 | GSK 2830371 | Sodium metatungstate | Idoxuridine | SF1670 | NSC 663284 | MSI-1436 lactate | BCI | D-erythro-Sphingosine | NSC-87877 | Razuprotafib
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