Nintedanib (free base)

BIBF-1120; BIBF1120

Yellow solid.

656247-17-5

32160000

liquid

GHS07

Protect from light and moisture.

InChI=1S/C31H33N5O4/c1-34-15-17-36(18-16-34)20-27(37)35(2)24-12-10-23(11-13-24)32-29(21-7-5-4-6-8-21)28-25-14-9-22(31(39)40-3)19-26(25)33-30(28)38/h4-14,19,32H,15-18,20H2,1-3H3,(H,33,38)/b29-28-

XZXHXSATPCNXJR-ZIADKAODSA-N

Chemical. CAS: 656247-17-5. Formula: C31H33N5O4. MW: 539.6. Nintedanib is an orally bioavailable and potent triple angiokinase inhibitor with potential antiangiogenic and antineoplastic activities. It targets the proangiogenic pathways mediated by the the receptor tyrosine kinases VEGFR1/2/3 (IC50=13-34nM), FGFR1/2/3 (IC50=37-108nM) and PDGFRalpha/beta (IC50=59-65nM), which may result in the induction of endothelial cell apoptosis, a reduction in tumor vasculature, and the inhibition of tumor cell proliferation and migration. Nintedanib competitively binds to the ATP binding-pocket of these receptors, resulting in interference with receptor dimerization and blocking intracellular signaling critical for the proliferation and survival of angiogenesis-related endothelial cells, pericytes and vascular smooth muscle cells. Nintedanib also inhibits some non-receptor kinases such as Fms-like tyrosine protein kinase (Flt-3, IC50=26nM), proto-oncogene ret (Ret, IC50=35nM), lymphocyte-specific tyrosine kinase (Lck, IC50=16nM), tyrosine-protein kinase lyn (Lyn, IC50=195nM) and proto-oncogene tyrosine protein kinase src (Src, IC50=156nM). Through this unique targeting profile nintedanib has significant antitumor activity in several tumor types.

MFCD11974012

C31H33N5O4

539.6

Vial

P261-P305+P351+P338

Nintedanib is an orally bioavailable and potent triple angiokinase inhibitor with potential antiangiogenic and antineoplastic activities. It targets the proangiogenic pathways mediated by the the receptor tyrosine kinases VEGFR1/2/3 (IC50=13-34nM), FGFR1/2/3 (IC50=37-108nM) and PDGFRalpha/beta (IC50=59-65nM), which may result in the induction of endothelial cell apoptosis, a reduction in tumor vasculature, and the inhibition of tumor cell proliferation and migration. Nintedanib competitively binds to the ATP binding-pocket of these receptors, resulting in interference with receptor dimerization and blocking intracellular signaling critical for the proliferation and survival of angiogenesis-related endothelial cells, pericytes and vascular smooth muscle cells. Nintedanib also inhibits some non-receptor kinases such as Fms-like tyrosine protein kinase (Flt-3, IC50=26nM), proto-oncogene ret (Ret, IC50=35nM), lymphocyte-specific tyrosine kinase (Lck, IC50=16nM), tyrosine-protein kinase lyn (Lyn, IC50=195nM) and proto-oncogene tyrosine protein kinase src (Src, IC50=156nM). Through this unique targeting profile nintedanib has significant antitumor activity in several tumor types.

>99% (HPLC)

Warning

O=C(OC)C1=CC=C2C(NC(/C2=C(NC3=CC=C(N(C(CN4CCN(C)CC4)=O)C)C=C3)/C5=CC=CC=C5)=O)=C1

Soluble in DMSO (5 mg/ml), DMF (10mg/ml) or ethanol (1mg/ml).

Non-hazardous

Biochemical Reagents

12352200

Stable for at least 2 years after receipt when stored at -20°C.