Henatinib maleate is t he 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. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

MedKoo Cat#: 205845 Name: Henatinib CAS#: 1239269-51-2 Chemical Formula: C25H29FN4O4 Exact Mass: 468.21728 Molecular Weight: 468.52056 Elemental Analysis: C, 64.09; H, 6.24; F, 4.05; N, 11.96; O, 13.66

Synonym: Henatinib

IUPAC/Chemical Name: (R,Z)-2-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-5-(2-hydroxy-3-morpholinopropyl)-3-methyl-5,6,7,8-tetrahydropyrrolo[3,2-c]azepin-4(1H)-one

InChi Key: MCTXSDCWFQAGFS-UEXNTNOUSA-N

InChi Code: InChI=1S/C25H29FN4O4/c1-15-22(12-19-18-11-16(26)4-5-20(18)28-24(19)32)27-21-3-2-6-30(25(33)23(15)21)14-17(31)13-29-7-9-34-10-8-29/h4-5,11-12,17,27,31H,2-3,6-10,13-14H2,1H3,(H,28,32)/b19-12-/t17-/m1/s1

SMILES Code: O=C1N(C[C@H](O)CN2CCOCC2)CCCC3=C1C(C)=C(/C=C4C(NC5=C4C=C(F)C=C5)=O)N3

Technical Data

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Additional Information

        

References

1: Gu P, Ding Y, Sun D, Hang T, Liu W, Ding L. Quantification of henatinib maleate, a novel potent inhibitor of VEGF receptors, in rat plasma by LC-MS/MS. Biomed Chromatogr. 2010 Apr;24(4):420-5. PubMed PMID: 19662624.