BIBF1120 (Vargatef, Nintedanib) is an oxindole-based, orally-available triple kinase inhibitor targeting the angiogenesis factors VEGF, PDGF, and FGF. It inhibits VEGFR, PDGFR, and FGFR at potency ranges of 13-34, 59-65, and 37-108 nM. [1] Kinase panel studies show that it also inhibits Flt-3, Lck, Lyn, and Src at 26, 16, 195, and 156 nM, respectively. BIBF1120 also inhibits cell proliferation in MAPK and Akt signaling pathways at EC50s of 10-80 nM.
Continuous oral QD dosing of BIBF1120 displayed antitumor activity in a number of tumor cell lines (FaDu, Caki-1, HT-29, SKOV-3, Calu-6, PAC-120, and GS-9L.
BIBF-1120 is being explored as a treatment for idiopathic pulmonary fibrosis and has shown promise in the delay of lung fibrosis progression. [2]
Technical information:
| Chemical Formula: | C31H33N5O4 | |
| CAS #: | 928326-83-4 | |
| Molecular Weight: | 539.62 | |
| Purity: | > 99% | |
| Appearance: | Yellow | |
| Chemical Name: | (Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate | |
| Solubility: | Up to 10 mM in DMSO | |
| Synonyms: | BIBF-1120, BIBF 1120, BIBF1120, Vargatef, Nintedanib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Hilberg et al., BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008, 68(12), 4774-4782. Pubmed ID: 18559524 |
| 2. | Antoniu, S., Nintedanib (BIBF 1120) for IPF: a tomorrow therapy? Multidiscip. Respir. Med. 2012, 7, 41-45. Pubmed ID: 23146151 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
