FRAX1036

SKU: orb1223304

Description

FRAX1036 is a potent and selective PAK1 inhibitor. Administration of docetaxel with either FRAX1036, or PAK1 small interfering RNA oligonucleotides dramatically altered signaling to cytoskeletal-associated proteins, such as stathmin, and induced microtubule disorganization and cellular apoptosis. Live-cell imaging revealed that the duration of mitotic arrest mediated by docetaxel was significantly reduced in the presence of FRAX1036, and this was associated with increased kinetics of apoptosis.

Key Properties

• CAS Number: 1432908-05-8
• MW: 518.05
• Purity: >98% (HPLC)
• Formula: C₂₈H₃₂ClN₇O
• SMILES: CCn1c2nc(ncc2cc(c1=O)c1c(cc(cc1)c1cncc(n1)C)Cl)NCCC1CCN(CC1)C
• Target: EGFR
• Solubility: DMSO : 5.3 mg/mL. 10.23 mM

Bioactivity

• In Vitro:
  FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively. FRAX1036 (2.5 μM) incombination with docetaxel alters stathmin phosphorylation, induces the apoptotic marker cleaved PARP and increases kinetics of apoptosis in MDA-MB-175 and HCC2911 cells; also alters microtubule organization, mitosis and cell fate in U2OS cells. Moreover, FRAX1036 shows significantly effective inhibition on U2OS cells. FRAX1036 (10 μM) affects the proliferation of non-small cell lung cancer (NSCLC) cells when added to KRAS prenylation inhibitors.

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

FRAX1036 | FRAX-1036 | FRAX 1036

Quick Database Links

Gene Symbol

EGFR