Cediranib
作者：齊岳
發布時間：2023-08-23
09:15:55
點擊數：
產品名稱：Cediranib
產品描述：
| 產品描述 | Cediranib (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells. |
| 靶點活性 | Flt1:5 nM, Flt4:≤3 nM |
| 體外活性 | Cediranib對人類移植瘤模型具有十分有效的作用且有劑量依賴性.此外,Cediranib可使人肺*移植瘤血管衰退.Cediranib使骨骼過度生長,對卵巢中黃體的產生具有阻礙作用,并抑制依賴于血管生成的生理程序. |
| 體內活性 | 在體外,Cediranib（微摩）可直接抑制細胞增殖。Cediranib（次納摩）阻斷細管產生,且對體內VEGF誘導的血管生成有抑制作用。Cediranib對bFGF（IC50：0.5 μM）和EGF（IC50：0.11 μM）有抑制作用。在MG63細胞系中,Cediranib抑制PDGF-AA（IC50：0.04 μM）。Cediranib抑制 Flt-1相關激酶（IC50：5 nM）,還對VEGF-C和VEGF-D受體Flt-4有抑制作用（IC50<3 nM）。此外,Cediranib對c-Kit（IC50：2 nM）和PDGFR-β（IC50：5 nM）酪氨酸激酶有抑制作用。 |
| 激酶實驗 | Kinase inhibition: Cediranib is dissolved in DMSO at a concentration of 10 mM. All enzyme assays are run at, or just below, the respective Km for ATP (0.2 - 30 μM). The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFRα, PDGFRβ, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aurora A, and Aurora B] using ELISA. Selectivity versus CDK2 and CDK4 serine/threonine kinases is examined using scintillation proximity assays with a retinoblastoma substrate and [γ-sup>33P]ATP. Activity of Cediranib is compared to MAPK kinase (MEK), which shows dual specificity. It is determined using a MAPK substrate, [γ-33P]ATP, and paper capture/scintillation counting. |
| 細胞實驗 | The proliferation of the HUVEC cell line is evaluated in the presence and absence of growth factors by measuring 3H-thymidine incorporation following a 4-day incubation period. Proliferation of MG63 osteosarcoma cells is induced by PDGF-AA, which selectively activates signaling of the PDGFRα homodimer. HUVEC and MG63 osteosarcoma cells are cultured in DMEM without phenol red containing 1% charcoal stripped FCS, 2 mM glutamine, and 1% nonessential amino acids for 24 hours. Cediranib or vehicle is added with PDGF-AA ligand (50 ng/mL) and plates incubated for another 72 hours. Cellular proliferation is determined using bromodeoxyuridine ELISA. (Only for Reference) |
| 別名 | AZD2171, NSC-732208, 西地尼布 |
| 分子量 | 450.514 |
| 分子式 | C25H27FN4O3 |
| CAS No. | 288383-20-0 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
DMSO: 83 mg/mL (184.2 mM)
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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