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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.
Cancer Res Commun. 2022 Aug.
Pharmacological inhibition of SHP2 blocks both PI3K and MEK signaling in low-epiregulin HNSCC via GAB1
SHP099 hydrochloride purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | non-small-cell lung cancer cells |
| Preparation method | Cells are plated onto 96-well plates in 100 μL medium. SHP099 with various concentrations (1.25, 2.5, 5, 10, 20 μM) are added 24 h after cell plating. At day 5, 50 μL Celltiter-Glo reagent is added, and the luminescent signal is determined |
| Concentrations | 1.25, 2.5, 5, 10, 20 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 388.72 |
| Formula | C16H20Cl3N5 |
| CAS Number | 1801747-11-4 |
| Solubility (25°C) | DMSO: 4 mg/mL (Need ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Phosphatase Products |
|---|
| RMC-3943
RMC-3943 is an allosteric SHP2 inhibitor (inhibition of full-length SHP2 in biochemical assay, IC50 = 2.19 nM). |
| LYP-IN-1
LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki and an IC50 of 110 nM and 0.259 μM, respectively. |
| PF-07284892
PF-07284892 (ARRY-558) is a potent and orally active SHP2 inhibitor with an IC50 value of 21 nM. |
| MY10
MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. |
| CPDA
CPDA is a novel potent SH2 domain-containing inositol phosphatase 2 (SHIP2) inhibitor. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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