Specifications
- Purity
- ≥99% (HPLC)
- Appearance
- Yellow solid
- Identity
- 1H-NMR
Properties
- Solvents
- DMSO (5 mg/ml), DMF (10 mg/ml) or ethanol (1 mg/ml).
Available from stock
Nintedanib (free base)
- SKU
- N0321
Categories:
- Synonyms
- BIBF-1120 , BIBF1120
- 656247-17-5
- CAS-Number
- C31H33N5O4
- Molecular Formula
- 539.6
- Molecular Weight
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
- Shipping
- AMBIENT
- Short Term Storage
- -20°C
- Long Term Storage
- -20°C
- Handling Advice
- Protect from light and moisture.
- Use / Stability
- Stable for at least 2 years after receipt when stored at -20°C.
- Hazard statements
- H302-H315-H319-H335
- Precautionary statements
- P261-P305+P351+P338
- GHS Symbol
- GHS07
- Signal word
- Warning
- Transportation
- Not dangerous goods
- Description
- 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 PDGFRα/β (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.
- Smiles
- 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
- InChi Key
- XZXHXSATPCNXJR-ZIADKAODSA-N
- References
- (1) F. Hilberg, et al., Cancer Res. 68, 4774 (2008) , (2) E.S. Santos, et al., Invest. New Drugs 30, 1261 (2012) (Review) , (3) C. Rolfo, et al., Expert Opin. Investig. Drugs 22, 1081 (2013) (Review) , (4) N. Awasthi & R.E. Schwarz, Onco. Targets Ther. 8, 3691 (2015) (Review)
- InChi
- 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-
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 PDGFRα/β (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.
Additional information
| Synonyms | BIBF-1120, BIBF1120 |
|---|---|
| Purity | ≥99% (HPLC) |
| Appearance | Yellow solid |
| CAS-Number | 656247-17-5 |
| Molecular Formula | C31H33N5O4 |
| Molecular Weight | 539.6 |
| Identity | 1H-NMR |
| Solvents | DMSO (5 mg/ml), DMF (10 mg/ml) or ethanol (1 mg/ml). |
| Smiles | 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 |
| InChi Key | XZXHXSATPCNXJR-ZIADKAODSA-N |
| Shipping | AMBIENT |
| Short Term Storage | -20°C |
| Long Term Storage | -20°C |
| Handling Advice | Protect from light and moisture. |
| Use / Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
| GHS Symbol | GHS07 |
| Signal word | Warning |
| Transportation | Not dangerous goods |
| References | (1) F. Hilberg, et al., Cancer Res. 68, 4774 (2008), (2) E.S. Santos, et al., Invest. New Drugs 30, 1261 (2012) (Review), (3) C. Rolfo, et al., Expert Opin. Investig. Drugs 22, 1081 (2013) (Review), (4) N. Awasthi & R.E. Schwarz, Onco. Targets Ther. 8, 3691 (2015) (Review) |
| InChi | 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- |
| Quantity | 25 mg, 100 mg, Bulk |
