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R1530

Catalog No. TQ0317 CAS 882531-87-5

Synonyms: antitumor, Inhibitor, Fibroblast growth factor receptor, mitosis, R-1530, FGFR, angiogenesis, R 1530, R1530, VEGFR, antiproliferative, Apoptosis, inhibit, mitotic, Vascular endothelial growth factor receptor

R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

R1530, CAS 882531-87-5

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Purity: 98%

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Description	R1530 is a multikinase inhibitor with antineoplastic and antiangiogenesis activities.
Targets&IC50	VGFR2:10 nM, FGFR1:28 nM
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 [1]. R1530 strongly inhibited human tumor cell proliferation. Growth factor-driven proliferation of endothelial and fibroblast cells was also inhibited [2].
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[2].

Synonyms	antitumor, Inhibitor, Fibroblast growth factor receptor, mitosis, R-1530, FGFR, angiogenesis, R 1530, R1530, VEGFR, antiproliferative, Apoptosis, inhibit, mitotic, Vascular endothelial growth factor receptor
Molecular Weight	356.78
Formula	C18H14ClFN4O
CAS No.	882531-87-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 5 mg/mL (14.01 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature

1. Tovar C, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75. 2. Kolinsky K, et al. Preclinical evaluation of the novel multi-targeted agent R1530. Cancer Chemother Pharmacol. 2011 Dec;68(6):1585-94.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

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