Henatinib - CAS 1239269-51-2
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Not Intended for Therapeutic Use. For research use only.
Henatinib maleate is the maleate salt form of henatinib, an orally bioavalable, multitargeted tyrosine kinase inhibitor with potential antitumor and antiangiogenic activities. Henatinib inhibits vascular endothelial growth factor receptor type 2 (VEGFR2), a tyrosine kinase receptor upregulated in many tumor cells that plays a key role in angiogenesis. This may result in an inhibition of angiogenesis and eventually tumor cell proliferation. Henatinib, structurally similar to sunitinib, also inhibits, though to a lesser extent, mast/stem cell growth factor receptor (c-Kit) and, platelet-derived growth factor receptor (PDGFR) alpha and beta.
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1.Quantification of henatinib maleate, a novel potent inhibitor of VEGF receptors, in rat plasma by LC-MS/MS.
Gu P1, Ding Y, Sun D, Hang T, Liu W, Ding L. Biomed Chromatogr. 2010 Apr;24(4):420-5. doi: 10.1002/bmc.1308.
Henatinib maleate (R,Z)-2-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene) methyl]-5-(2-hydroxy-3-morpholinopropyl)-3-methyl-5,6,7,8-tetrahydro-1H-pyrrolo[3,2-c] azepin-4-ketone maleate is a potent inhibitor of vascular endothelial growth factor receptors, and is currently under preclinical evaluation as an anticancer drug. A novel method for the quantification of henatinib maleate in rat plasma using high performance liquid chromatography-tandem mass spectrometry has been developed. The analyte (henatinib maleate) and internal standard (papaverine hydrochloride) were extracted from 50 microL of rat plasma by protein precipitation and separated on a C(18) column using a mixture of 25 mm ammonium acetate buffer : methanol : acetonitrile (35 : 50 : 15, v/v/v) as mobile phase with a run time of 4.5 min. The detection was performed by means of triple quadrupole mass spectrometer equipped with an ESI interface operating in the multiple-reaction monitoring mode.
2.Determination of henatinib in human plasma and urine by liquid chromatography-tandem mass spectrometry and its pharmacokinetic application.
Qian J1, Wang Y, Cao J, Li J. J Pharm Biomed Anal. 2013 Jun;80:173-9. doi: 10.1016/j.jpba.2013.03.010. Epub 2013 Mar 26.
Henatinib is a novel oral small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities in preclinical studies. In support of a clinical pharmacokinetic study, a simple, sensitive and rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of henatinib in human plasma and urine. The sample preparation procedure involved a simple protein precipitation with methanol and the addition of midazolam as the internal standard. The chromatographic separation was achieved on an XBridge C18 column (50mm×2.1mm, 2.5μm) using a mixture of 5mM ammonium formate (pH 9.5)-acetonitrile-methanol (60:30:10, v/v/v) as the mobile phase. The MS/MS detection was performed in the positive ion multiple reaction monitoring (MRM) mode by monitoring the precursor→product ion transitions at m/z 469.1→382.2 for henatinib and m/z 326.2→291.3 for the internal standard. Assays were validated over the concentration range of 0.
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CAS 1239269-51-2 Henatinib

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