Henatinib - CAS 1239269-51-2
Catalog number:
1239269-51-2
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
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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Synonyms:
Henatinib
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Current Developer:
Jiangsu HengRui Medicine Co., Ltd
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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