R1530

SKU: orb1296058

Description

R1530 is a small molecule multikinase inhibitor exhibiting both antitumor and antiangiogenic properties. It is utilized in cancer research, with studies demonstrating its activity in inhibiting tumor growth and angiogenesis in both cellular and animal models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 882531-87-5
• MW: 356.78
• Purity: 98.42%
• Formula: C₁₈H₁₄ClFN₄O
• SMILES: COc1cc2N=C3NNC(C)=C3N=C(c3ccccc3Cl)c2cc1F
• Target: Apoptosis,VEGFR,FGFR,FLT,PDGFR
• Solubility: DMSO:5 mg/mL (14.01 mM)

Bioactivity

• Target IC50:
  VGFR2:10 nM|FGFR1:28 nM
• In Vivo:
  Showing significant tumor growth inhibition in a lung cancer xenograft model, R1530 was administered at doses ranging from once daily, weekly and twice weekly (3.125-50 mg/kg qd, 100 mg/kg qw, 100 mg/kg kg biw). Tumor regression occurred in all models treated with the maximum tolerated daily dose (50 mg/kg). Doses of 25 and 50 mg/kg qd resulted in biologically significant increases in survival in all models tested. After oral administration to nude mice, R1530 showed good tissue permeability. Exposure was dose-dependent, up to 100 mg/kg when administered orally.
• In Vitro:
  R1530 inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as VEGFR-1/2/3, PDGFR, Flt-3, and FGFR-1/2. In the presence of R1530, polyploid cancer cells underwent apoptosis or became senescent which translated into potent in vitro and in vivo efficacy. Normal proliferating cells were resistant to R1530-induced polyploidy. Mitotic checkpoint kinase BubR1 was found downregulated during R1530-induced exit from mitosis, a likely consequence of PLK4 inhibition . R1530 strongly inhibited human tumor cell proliferation. Growth factor-driven proliferation of endothelial and fibroblast cells was also inhibited .

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

R1530, R-1530, R 1530, VEGFR1, VEGFR, VEGFR2, Vascular endothelial growth factor receptor, VEGFR3, FLT3, FGFR2, Fibroblast growth factor receptor, FGFR1, FGFR, Inhibitor, inhibit, PDGFR, mitosis, mitotic, antitumor, antiproliferative, Apoptosis, angiogenesis

Compound Identifiers

PubChem CID

135398512