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SHP099 hydrochloride

Catalog No. T3544   CAS 2200214-93-1

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
SHP099 hydrochloride Chemical Structure
SHP099 hydrochloride, CAS 2200214-93-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
5 mg In stock $ 71.00
10 mg In stock $ 98.00
25 mg In stock $ 177.00
50 mg In stock $ 259.00
100 mg In stock $ 475.00
500 mg In stock $ 1,050.00
1 g In stock $ 1,390.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 99.62%
Purity: 99.28%
Purity: 99.27%
Purity: 99.13%
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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 SHP2:70 nM.
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 exhibits inhibition of cell proliferation (KYSE-520 model) with an IC50 of 1.4 μM. SHP099 also exhibits high solubility and high permeability with no apparent efflux in Caco-2 cells[1]. SHP099 concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, therefore, inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signaling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells[2].
In vivo Dose-dependent exposure and modulation of the pharmacodynamic marker p-ERK was observed in xenografts following single doses of 30 and 100 mg/kg (red and blue lines, respectively). 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. 2200214-93-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Methanol: 15 mg/mL (38.59 mM), sonification is recommended.

DMSO: 55 mg/mL (141.49 mM), Sonification/heating is recommended.

H2O: 10 mg/mL (25.73 mM), Sonification is recommended

TargetMolReferences 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.

TargetMolCitations

1. Qiu W Q, Ai W, Zhu F D, et al. Polygala saponins inhibit NLRP3 inflammasome-mediated neuroinflammation via SHP-2-Mediated mitophagy. Free Radical Biology and Medicine. 2022, 179: 76-94. 2. Zheng M, Liu Y, Wu C, et al. Novel PROTACs for degradation of SHP2 protein. Bioorganic Chemistry. 2021, 110: 104788

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Highly Selective Inhibitor Library NO PAINS Compound Library Phosphatase Inhibitor Library Glycometabolism Compound Library Autophagy Compound Library Lipid Metabolism Compound Library Anti-Cancer Compound Library Metabolism Compound Library Preclinical Compound Library

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Keywords

SHP099 hydrochloride 2200214-93-1 Metabolism Others Phosphatase SHP-099 SHP099 Hydrochloride SHP 099 Inhibitor SHP 099 Hydrochloride inhibit SHP-099 Hydrochloride SHP-099 hydrochloride SHP099 inhibitor

 

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