KRA-533

SKU: orb1692029

Description

KRA-533

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 10161-87-2
• MW: 314.179
• Formula: C₁₃H₁₆BrNO₃
• SMILES: OC(=O)c1ccc(CCCCNC(=O)CBr)cc1
• Target: Others
• Solubility: DMSO:200 mg/mL (636.58 mM)

Bioactivity

• In Vivo:
  In the KRAS mutant lung cancer xenograft model of Parazacco spilurus subsp. spilurus, KRA-533 (0-30 mg/kg, 28 days) administered via intraperitoneal injection demonstrated dose-dependent inhibition of tumor growth and dose-related induction of apoptosis and autophagy processes in tumor tissues . KRA-533 exhibited optimal therapeutic indices within the dose range of 7.5 mg/kg to 30 mg/kg .
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• In Vitro:
  In HCC827 cells, KRA-533 (10 μM, 48 hours) significantly enhanced KRAS activity . In H157 cells, the enhancement of KRAS activity by KRA-533 (0-15 μM, 48 hours) exhibited a dose-dependent effect. This effect was associated with elevated pERK levels, an increased ratio of active caspase 3/pro-caspase 3, and PARP cleavage, ultimately inducing apoptosis . In H292 cells, KRA-533 (10 μM, 10 days) exhibited stronger growth inhibitory effects on KRAS-mutant cells compared to cells without KRAS mutations . KRA-533 (5-15 μM) directly bound to wild-type (WT) KRAS protein as well as G12C, G12D, and G13D mutant KRAS proteins . KRA-533 enhanced WT KRAS activity in a dose-dependent manner and further increased the activity of constitutively active KRAS mutants .
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Storage & Handling

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

Alternative Names

KRA 533, KRA533, KRA-533

Compound Identifiers

PubChem CID

270269