Nintedanib (BIBF 1120) | CAS#656247-17-5APExBIO貨號 A8252
VEGFR/PDGFR/FGFR inhibitor-Nintedanib (BIBF 1120)
Nintedanib (BIBF 1120)| CAS#656247-17-5APExBIO貨號 A8252
SIRT1 activator Purity: 97.22%
尼達尼布(Nintedanib, BIBF 1120) 是一種吲哚酮衍生(indolinone-derived)的口服活性三重血管激酶抑制劑，血管內皮生長因子受體( vascular endothelial growth factor receptor, VEGFR)1-3、纖維母細胞生長因子受體(fibroblast growth factor receptor, FGFR)1-3和血小板衍生生長因子受體( platelet-derived growth factor receptor, PDGFR)α /β1。它透過阻斷這些受體介導的信號通路，在納摩爾濃度（IC50，20-100 nmol/L）下顯示出有效的抗血管生成活性。尼達尼布(Nintedanib, BIBF 1120) 正處於治療特發性肺纖維化( idiopathic pulmonary fibrosis)的臨床開發階段，因為這些受體已被證明可能參與肺纖維化的發病機制。作為一種新型血管生成抑制劑( novel angiogenesis inhibitor)，它也在不同的癌症模型中得到廣泛評估，並透過抑制腫瘤血管形成表現出顯著的抗腫瘤活性。
為了進一步評估其對多種腫瘤的抗腫瘤作用，尼達尼布(Nintedanib, BIBF 1120)目前正在進入多項臨床試驗，包括非小細胞肺癌(non-small cell lung cancer)、卵巢癌(ovarian cancer)、大腸癌(colorectal cancer)、肝細胞癌(hepatocellular carcinoma)和許多其他實體瘤 (solid tumors)。此外，尼達尼布療法與多西他賽和阿法替尼等其他療法相結合的可能性正在不同的腫瘤模型中進行測試。患者最常見的藥物相關不良事件是腹瀉 (diarrhea)、噁心 (nausea)、嘔吐( vomiting)和嗜睡(lethargy)。
- 1. da Silva RF, Banzato TP, et al. “Antiangiogenic therapy with Nintedanib affects hypoxia, angiogenesis and apoptosis in the ventral prostate of TRAMP animals.” Cell Tissue Res. 2019 Aug 31. PMID:31473819
- 2. Mateus PAM, Kido LA, et al. “Association of anti-inflammatory and antiangiogenic therapies negatively influences prostate cancer progression in TRAMP mice.” Prostate. 2018 Dec 25. PMID:30585351
- 3. Pangrazi EN, da Silva RF, et al. “Nintedanib treatment delays prostate dorsolateral lobe cancer progression in the TRAMP model: Contribution to the epithelial-stromal interaction balance.” Cell Biol Int. 2017 Oct 5. PMID:28980742
- 4. Janelle DeJong.”Determination of Anti-Fibrotic Effects of Possible Scar-Collagen Antagonists on TGF-β1 Treated Dermal Fibroblasts.” 2017 Feb 1;7(2):203-217. eCollection 2017.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 539.62 |
| Cas No. | 656247-17-5 |
| Formula | C31H33N5O4 |
| Synonyms | Vargatef |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥5.34 mg/mL in DMSO |
| Chemical Name | methyl (3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylate |
| SDF | Download SDF |
| Canonical SMILES | CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)NC(=C3C4=C(C=C(C=C4)C(=O)OC)NC3=O)C5=CC=CC=C5 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
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| A4180 | A4180-5 | SRT1720 HCl | 1001645-58-4 | SIRT1 activator |
| A4182 | A4182-5.1 | Resveratrol | 501-36-0 | SIRT1 activator |