SHP099 hydrochloride
CAS No. : 1801747-11-4

Size Stock Price Quantity Add to Cart Quotation Online
1mg In-stock USD 60.0
5mg In-stock USD 84.0
10mg In-stock USD 120.0
50mg In-stock USD 288.0
100mg In-stock USD 528.0
Products are for research use only. Not for human use. We do not sell to patients.

Bulk Inquiry

Your information is safe with us. * Required Fields
* Country or Region:
* Applicant name:
* Organization Name:
* Email address:
* Requested quantity:
* Phone number:
Organization name, 
Email address, 
Requested quantity, 
Phone number, 
  • Data Sheet

  • Introduction

  • SDS

  • COA & Spectra

Name: SHP099 hydrochloride; 
Cat. No. : CS-5685
CAS No. : 1801747-11-4
Formula: C16H20Cl3N5
M. Wt. : 388.72
Solubility: DMSO: 4.1 mg/mL; H2O: 7.69 mg/mL (Need ultrasonic and warming)


SHP099 hydrochloride is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM. IC50 & Target: IC50: 70 nM (SHP2)[1] 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[1]. 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[2]. 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[1].


Kinase Assay: [1]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 Assay: [1]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].


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.

Chen YN, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52.

Enter Lot Number:

We apologize for the inconvenience. The Certificate of Analysis you requested is not currently available on-line:

1. The Lot Number you requested may have been entered incorrectly. How to get a Lot Number

2. The COA of the Lot you requested has not been added to our database.

Browsing History
    Other Forms
    Tags:SHP099 hydrochloride supplier,SHP099 hydrochloride purchase,SHP099 hydrochloride manufacturer,SHP099 hydrochloride sigma,SHP099 hydrochloride distributor,cost,SHP099 hydrochloride buy,SHP099 hydrochloride for sale
    Please enter your email address
    Organization name: Email:

    Submit success

    No information on this batch number
    How to get a Lot Number

    Lot numbers can be found on the outside label of a product:

    ChemScene Label