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My CartCAS：656247-18-6
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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| CAS | 656247-18-6 |
| Name | Nintedanib Ethanesulfonate Salt |
| Molecular Formula | C33H39N5O7S |
| Molecular Weight | 649.76 |
| Solubility | Soluble in Water/DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD26142360 |
| Target Point | VEGFR1/2/3;FGFR1/2/3 ;PDGFR |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background | It is a potent triple inhibitor of VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β. |
| Biological Activity | Nintedanib Ethanesulfonate Salt 是一种强效的三重血管激酶抑制剂，对 VEGFR1/2/3、FGFR1/2/3 和 PDGFRα/β 的 IC50 分别为 34 nM/13 nM/13 nM、69 nM/37 nM/108 nM 和 59 nM/65 nM。[1] |
| IC50 | VEGFR1: 34nM(IC50);VEGFR2: 13nM(IC50);VEGFR3: 13nM(IC50);FGFR1: 69nM(IC50);FGFR2: 37nM(IC50);FGFR3: 108nM(IC50);PDGFRα: 9nM(IC50);PDGFRβ: 65nM(IC50) [1] |
| In Vitro | BIBF 1120 is an indolinone derivative potently blocking VEGF receptor(VEGFR)，PDGFR and FGFR kinase activity in enzymatic assays(IC(50)，20-100 nmol/L). BIBF 1120 inhibits mitogen-activated protein kinase and Akt signaling pathways in three cell types contributing to angiogenesis，endothelial cells，pericytes，and smooth muscle cells，resulting in inhibition of cell proliferation(EC(50)，10-80 nmol/L)and apoptosis.[1] The combination of trifluridine and nintedanib exerted an additive effect on the growth inhibition of DLD-1 and HT-29 cells and a sub-additive effect on HCT116 cells.[2] |
| In Vivo | In human tumor xenografts growing in nude mice and a syngeneic rat tumor model，BIBF 1120 is highly active at well-tolerated doses(25-100 mg/kg daily p.o.)reducing vessel density and vessel integrity after 5 days，and inducing profound growth inhibition.[1] In the human colorectal cancer cell lines nude mice，the tumor growth inhibition with combination therapy of TFTD(150 mg/kg/day，orally administered，1-14 days)and/or nintedanib(40 mg/kg/day，orally administered，1-14 days)was 61.5，72.8，67.6 and 67.5% for the DLD-1，DLD-1/5-FU，HT-29，and HCT116 xenografts，respectively. This was significantly(P<0.05)higher than the effects of monotherapy with either TFTD or nintedanib.[2] |
| Data Literature Source | [1]. Hilberg F，et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. [2]. Suzuki N，et al. Effect of a novel oral chemotherapeutic agent containing a combination of trifluridine，tipiracil and the novel triple angiokinase inhibitor nintedanib，on human colorectal cancer xenografts. Oncol Rep. 2016 Dec;36(6):3123-3130. |
| Unit | Bottle |
| Specification | 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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