BRAF inhibitor 13

SKU: orb1227002

Description

A potent and selective B-Raf inhibitor with IC50 of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively; induces proliferation and hyperplasia in normal tissues of mice.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1093100-40-3
• MW: 478.944
• Purity: >98% (HPLC)
• Formula: C₂₆H₁₉ClN₈
• SMILES: CC1=C(C2=C(C=C1)C(=NC=C2)NC3=CC=C(C=C3)Cl)NC4=C(C=CC=N4)C5=C6C(=NC=N5)N=CN6
• Target: Raf
• Solubility: DMSO: ≥53 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vitro:
  Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. Raf inhibitor 1 (Compound 13) binds to and stabilizes B-Raf in a DFG-out, inactive conformation in which the ATP pocket is partially filled by Phe595 and Gly596 from the DFG motif. Raf inhibitor 1 (Compound 13) additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers.
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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

BRAF-IN-13

Quick Database Links

Gene Symbol

Raf