CGP77675

SKU: orb1304556

Description

CGP77675 (ZINC1488120) is a potent, selective Src family kinase inhibitor, demonstrating IC50 values of 5-20 nM for peptide substrate phosphorylation and 40 nM for Src autophosphorylation. Its anticancer activity supports its use in vitro and in vivo for researching cancer cell signaling, proliferation, and metastasis.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 234772-64-6
• MW: 443.54
• Purity: 99.66% (May vary between batches)
• Formula: C₂₆H₂₉N₅O₂
• SMILES: NC1=C2C(=CN(C2=NC=N1)C3=CC=C(CCN4CCC(O)CC4)C=C3)C5=CC(OC)=CC=C5
• Target: Bcr-Abl,VEGFR,EGFR,Src
• Solubility: DMSO:55 mg/mL (124 mM);10% DMSO+90% Saline:2.5 mg/mL (5.64 mM)

Bioactivity

• Target IC50:
  v-ABL:0.31 μM (IC50)|Lck:0.29 μM (IC50)|Src:0.02 μM (IC50)|EGFR:0.15 μM (IC50)|KDR:1.0 μM (IC50)
• In Vivo:
  In female rats of the Sprague-Dawley-derived strain Tif:RAlf, CGP77675 (10 and 50 mg/kg;orally) partially prevents bone loss and rescues bone microarchitectural features. In male mice, CGP77675 (1, 5, and 25 mg/kg; s.c.) inhibits IL-1β-induced hypercalcemia without affecting serum amyloid protein levels.
• In Vitro:
  CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 20, 150, 1000, 310, and 290 nM, respectively. CGP77675 dose-dependently inhibits phosphorylation of poly-Glu-Tyr (IC50 = 5.5 nM), and of the optimal Src substrate (OSS) peptide (IC50 = 16.7 nM). In rat fetal long bone cultures, CGP77675 inhibits the parathyroid hormone-induced bone resorption (IC50 = 0.8 μM). In Src-overexpressing IC8.1 cells, CGP77675 (0.04-10 μM) dose-dependently inhibits phosphorylation of Fak (IC50 = 0.2 μM) and paxillin(IC50 = 0.5 μM), but not of Src(IC50 = 5.7μM).

Storage & Handling

• Storage: 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

ZINC 1488120, ZINC1488120, ZINC-1488120, Src, v-Abl, EGFR, Lck, KDR, BcrAbl, 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol, CGP77675, CGP-77675, CGP 77675

Compound Identifiers

PubChem CID

5311381