1. Protein Tyrosine Kinase/RTK
  2. Discoidin Domain Receptor

SHP099 

Cat. No.: HY-100388 Purity: 99.56%
Handling Instructions

SHP099 is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM.

For research use only. We do not sell to patients.
SHP099 Chemical Structure

SHP099 Chemical Structure

CAS No. : 1801747-42-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 84 In-stock
1 mg USD 60 In-stock
5 mg USD 108 In-stock
10 mg USD 180 In-stock
50 mg USD 540 In-stock
100 mg USD 768 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of SHP099:

    SHP099 purchased from MCE. Usage Cited in: Open Biol. 2017 May;7(5). pii: 170066.

    Comparing the effects of SHP2 degradation and allosteric inhibition on Ras/MAPK signalling. (a) Human U2OS, A549, K-562 and MDA-MB-468 cells are treated with DMSO control or 1, 5 and 10 µM SHP099 for 2 h prior to lysis. Extracts (10 µg protein) are resolved by SDS-PAGE and transferred to nitrocellulose membranes, which are subjected to western blotting with the indicated antibodies. (b) Uninfected U2OS cells (WT) or cells infected with retroviruses encoding VHL, aCS3 and VHL-aCS3 are treated wit

    SHP099 purchased from MCE. Usage Cited in: Hepatology. 2018 Jan 23.

    Primary human HSCs are treated with SHP099 for 1 hour. PDGF-BB is added and cells are cultured for 12 additional hours. Whole cell lysates and EVs are examined by WB (n=6).

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    SHP099 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].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.8388 mL 14.1941 mL 28.3881 mL
    5 mM 0.5678 mL 2.8388 mL 5.6776 mL
    10 mM 0.2839 mL 1.4194 mL 2.8388 mL
    Please refer to the solubility information to select the appropriate solvent.
    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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    352.26

    Formula

    C₁₆H₁₉Cl₂N₅

    CAS No.

    1801747-42-1

    SMILES

    NC1=NC(N2CCC(C)(N)CC2)=CN=C1C3=CC=CC(Cl)=C3Cl

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 6.4 mg/mL (Need ultrasonic)

    SHP099 is dissolved in 5%DMSO[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.56%

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    Inquiry Information

    Product Name:
    SHP099
    Cat. No.:
    HY-100388
    Quantity: