SHP099 hydrochloride

SKU: orb1304082

Description

SHP099 hydrochloride is a potent and selective oral SHP2 inhibitor with an IC50 of 70 nM. It effectively blocks downstream ERK1/2 signaling in cancer cells and is widely used in vitro and in vivo to study oncogenic pathways in cancers driven by RTK or RAS signaling.

Research Area

Metabolism Research

Key Properties

• CAS Number: 2200214-93-1
• MW: 388.72
• Purity: 99.68% (May vary between batches)
• Formula: C₁₆H₂₀Cl₃N₅
• SMILES: Cl.CC1(N)CCN(CC1)c1cnc(c(N)n1)-c1cccc(Cl)c1Cl
• Target: Phosphatase
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (6.43 mM);Methanol:15 mg/mL (38.59 mM);DMSO:32 mg/mL (82.32 mM);H2O:10 mg/mL (25.73 mM)

Bioactivity

• Target IC50:
  SHP2:70 nM.
• In Vivo:
  METHODS: The imiquimod (IMQ)-induced mouse psoriasis model was treated with SHP0999 (1, 3, 10 mg/kg), and the effect of SHP099 on the psoriasis-like phenotype in the IMQ-induced mouse model was observed. . RESULTS SHP099 significantly inhibited IMQ-induced swelling, epidermal acanthosis, keratinocyte proliferation and dermal inflammatory cell infiltration without affecting the skin condition of normal mice; SHP099 also significantly reduced serum IL-23 and IL in the mouse model -17A level. METHODS: The ability of SHP099 to cross the BBB in C57BL/6J mice was evaluated after a single oral dose of SHP099 at 100 mg/kg in a 400 μL volume. RESULTS SHP099 concentrations were high in plasma and brain tissue early after oral gavage, and SHP099 levels in brain tissue remained at appreciable levels 24 h after oral gavage. METHODS: CT-26 and MC-38 cells were subcutaneously inoculated into BALB/c mice to establish a mouse tumor model. The mouse tumor model used SHP099 hydrochloride (5 mg/kg/kg/d, intraperitoneal injection). SHP099 salt was observed. Effects of salt on tumors. RESULTS The volume and weight of tumors treated with SHP099 were significantly reduced.
• In Vitro:
  METHODS: Cell viability of SMSCs was observed after treatment with different concentrations of SHP099 (5, 10, 15, 20, 25, 30, 40, 50 μM) for 1 week. RESULTS SHP099 inhibited the cell viability of SMSCs at concentrations greater than 25 μM.
• 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.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, SHP 099, SHP 099 Hydrochloride, SHP099 Hydrochloride, SHP099 hydrochloride, SHP-099 Hydrochloride, SHP-099 hydrochloride, SHP099, SHP-099, SHP-2, Phosphatase

Compound Identifiers

PubChem CID

121241170