A multi-kinase inhibitor
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R 1530

Item No. 15255

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl-pyrazolo[3,4-b][1,4]benzodiazepine
CAS Number
882531-87-5
Molecular Formula
C18H14ClFN4O
Formula Weight
356.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 30 mg/mLDMSO:PBS (pH 7.2) (1:7): 0.12 mg/mLEthanol: 20 mg/mL
λmax
254, 395 nm
SMILES
COC(C(F)=C1)=CC2=C1C(C3=CC=CC=C3Cl)=NC4=C(C)NN=C4N2
InChi Code
InChI=1S/C18H14ClFN4O/c1-9-16-18(24-23-9)21-14-8-15(25-2)13(20)7-11(14)17(22-16)10-5-3-4-6-12(10)19/h3-8H,1-2H3,(H2,21,23,24)
InChi Key
UOVCGJXDGOGOCZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    R 1530 is a multi-kinase inhibitor that targets over 20 kinases, including angiogenesis-related receptor tyrosine kinases (Kds = 61, 88, and 15 nM for FGFR1, PDGFRβ, and VEGFR2, respectively).1 It also inhibits FLT1, KIT, PLK4, and RET with Kd values of 9, 26, 11, and 22 nM, respectively.1 In cells, R 1530 delays mitosis, induces polyploidy, and blocks angiogenesis, ultimately promoting apoptosis or senescence.1,2 R 1530 strongly inhibits human tumor cell proliferation and reduces the growth of tumors in cancer xenograft models.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, J.-J., Higgins, B., Ju, G., et al. Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors. ACS Med. Chem. Lett. 4(2), 259-263 (2013).

    2. Tovar, C., Higgins, B., Deo, D.D., et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle 9(16), 3364-3375 (2010).

    3. Kolinsky, K., Tovar, C., Zhang, Y.-E., et al. Preclinical evaluation of the novel multi-targeted agent R1530. Cancer Chemother. Pharmacol. 68(6), 1585-1594 (2011).