CCT196969

SKU: orb1226891

Description

CCT196969 is a potent, orally bioavailable pan-RAF inhibitor with IC50 of 100, 40 and 12 nM for B-Raf, B-Raf V600E and C-Raf, respectively; also potently inhibits SRC (IC50=26 nM) and LCK (IC50=14 nM), does not inhibit MEK1 or the MEK1 kinase COT; inhibits cell proliferation of BRAF-selective-inhibitor-resistant cells with mean GI50 of 0.4 uM, NRAS mutant melanoma cells (GI50=0.6 uM); induces caspase 3 and PARP cleavage, induces apoptosis, inhibits the growth of PLX4720-resistant A375 xenografts (A375/R) in mice, without causing any body weight loss.

Key Properties

• CAS Number: 1163719-56-9
• MW: 513.5229
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₄FN₇O₃
• SMILES: FC1=CC(OC2=C3C(NC(C=N3)=O)=NC=C2)=CC=C1NC(NC4=CC(C(C)(C)C)=NN4C5=CC=CC=C5)=O
• Target: Raf
• Solubility: DMSO: ≥ 32 mg/mL

Bioactivity

• In Vivo:
  CCT196969 is extremely well tolerated and does not produce any significant adverse effects In vivo. It inhibits the growth of NRAS mutant DO4 tumor xenografts in nude mice. CCT196969 inhibits ERK and SRC and induce tumor regression in a PDX from the resistant tumor without causing body weight loss in the mice.
• In Vitro:
  CCT196969 is a pan-Raf inhibitor with anti-SRC activity. CCT196969 is an orally available, well-tolerated B-Raf inhibitor that directly inhibits B-RafV600E in cells. CCT196969 inhibits B-Raf at 100 nM and B-RafV600E at 40 nM. It inhibits CRaf at 12 nM, SRC at 26 nM, and LCK at 14 nM. CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for B-Raf. CCT196969 induces caspase 3 and PARP cleavage, demonstrating that it induces apoptosis.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CCT-196969 | CCT 196969

Quick Database Links

Gene Symbol

Raf