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Metabolism Phosphatase SHP099 hydrochloride

SHP099 hydrochloride

Catalog No. T3544   CAS 1801747-11-4

SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor.

SHP099 hydrochloride, CAS 1801747-11-4
Pack Size Availability Price/USD Quantity
1 mg In stock 36.00
5 mg In stock 84.00
10 mg In stock 154.00
50 mg In stock 520.00
100 mg In stock 815.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor.
Targets&IC50 SHP-2 : ic50 70nM,   SHP2 : ic50 70 nM.,  
In vitro 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].
Kinase Assay The inhibition of SHP2 from the tested compounds (SHP099) concentrations varying from 0.003-100 μM is monitored using an assay in which 0.5 nM of SHP2 is incubated with of 0.5 μM of peptide IRS1_pY1172(dPEG8)pY1222. After 30-60 minutes incubation at the surrogate substrate, DiFMUP is added to the reaction and incubated at 25 °C for 30 minutes. The reaction is then quenched by the addition of 5 μL of a 160 μM solution of bpV(Phen). The fluorescence signal is monitored using a microplate reader using excitation and emission wavelengths of 340 nm and 450 nm, respectively[1].
Cell Research
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[1].
Molecular Weight 388.72
Formula C16H20Cl3N5
CAS No. 1801747-11-4

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

H2O: 2.5 mg/mL (6.43 mM)

DMSO: 4.1 mg/mL (10.55 mM), Need ultrasonic and warming

Methanol: 15 mg/mL (38.59 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52. 3. Carmine Fedele, et al. SHP2 Inhibition Abrogates MEK inhibitor Resistance in Multiple Cancer Models. bioRxiv. April 25, 2018. 4. Carmine Fedele, et al. SHP2 Inhibition Abrogates MEK inhibitor Resistance in Multiple Cancer Models. bioRxiv. April 25, 2018.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Autophagy Compound Library MAPK Inhibitor Library Phosphatase Inhibitor Library

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