CCT196969

SKU: orb1303113

Description

CCT196969

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1163719-56-9
• MW: 513.52
• Purity: 99.65%
• Formula: C₂₇H₂₄FN₇O₃
• SMILES: CC(C)(C)c1cc(NC(=O)Nc2ccc(Oc3ccnc4[nH]c(=O)cnc34)cc2F)n(n1)-c1ccccc1
• Target: Raf,Src
• Solubility: H2O:Insoluble;DMSO:127.5 mg/mL (248.29 mM);Ethanol:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.79 mM)

Bioactivity

• Target IC50:
  Src:0.03 μM|B-Raf (V600E):0.04 μM|Lck:0.02 μM|B-Raf:0.1 μM|Raf:0.01 μM
• In Vivo:
  Oral dosing at 10 mg/kg/day of CCT196969 results in plasma concentrations ～1 μM at 24 hr. It is orally bioavailable at ～55%. CCT196969 is extremely well tolerated at the doses assessed and does not produce any significant adverse effects in vivo.
• In Vitro:
  CCT196969 induces caspase 3 and PARP cleavage, thus induces apoptosis. CCT196969 does not drive paradoxical pathway activation and inhibit MEK/ERK in BRAF and NRAS mutant melanoma. CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for BRAF, but not cancer cells that are wild-type for BRAF and NRAS.
• Cell Research:
  Cell lines: cell line derived from a vemurafenib-resistant melanoma. Method: The three cell lines derived from tumors displaying resistance to vemurafenib are incubated with DMSO (control),PLX4720,CCT196969,or CCT241161 (1 μM; 4 hr).Protein extracts are prepared in CLB1 lysis buffer,and samples are analyzed by Zeptosens RPPA(reverse phase protein arrays).
• Animal Research:
  Animal Models: CD-1 mice. Formulation: 5% DMSO,95% water. Dosages: 20 mg/kg . Administration: oral gavage

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

inhibit, Inhibitor, CCT196969, CCT-196969, CCT 196969, C-RAF, Src, Raf, Raf kinases

Compound Identifiers

PubChem CID

42628843