Cediranib
作者：齊岳
發(fā)布時(shí)間：2023-08-23
09:15:55
點(diǎn)擊數(shù)：
產(chǎn)品名稱(chēng)：Cediranib
產(chǎn)品描述：
| 產(chǎn)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(diǎn)活性 | Flt1:5 nM, Flt4:≤3 nM |
| 體外活性 | Cediranib對(duì)人類(lèi)移植瘤模型具有十分有效的作用且有劑量依賴(lài)性.此外,Cediranib可使人肺癌移植瘤血管衰退.Cediranib使骨骼過(guò)度生長(zhǎng),對(duì)卵巢中黃體的產(chǎn)生具有阻礙作用,并抑制依賴(lài)于血管生成的生理程序. |
| 體內(nèi)活性 | 在體外,Cediranib（微摩）可直接抑制腫瘤細(xì)胞增殖。Cediranib（次納摩）阻斷細(xì)管產(chǎn)生,且對(duì)體內(nèi)VEGF誘導(dǎo)的血管生成有抑制作用。Cediranib對(duì)bFGF（IC50：0.5 μM）和EGF（IC50：0.11 μM）有抑制作用。在MG63細(xì)胞系中,Cediranib抑制PDGF-AA（IC50：0.04 μM）。Cediranib抑制 Flt-1相關(guān)激酶（IC50：5 nM）,還對(duì)VEGF-C和VEGF-D受體Flt-4有抑制作用（IC50<3 nM）。此外,Cediranib對(duì)c-Kit（IC50：2 nM）和PDGFR-β（IC50：5 nM）酪氨酸激酶有抑制作用。 |
| 激酶實(shí)驗(yàn) | 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(xì)胞實(shí)驗(yàn) | 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(chǔ)
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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