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Cediranib maleate (AZD-2171 maleate) Sale

(Synonyms: 西地尼布马来酸盐; AZD-2171 maleate) 目录号 : GC33004

An inhibitor of VEGF receptor tyrosine kinases

Cediranib maleate (AZD-2171 maleate) Chemical Structure

Cas No.:857036-77-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥561.00
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5mg
¥450.00
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10mg
¥675.00
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50mg
¥2,160.00
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100mg
¥3,420.00
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Sample solution is provided at 25 µL, 10mM.

Description

Receptors for VEGF have central roles in vasculogenesis and angiogenesis and thus serve as targets for cancer therapy.1,2 Cediranib is a potent inhibitor of VEGF receptor tyrosine kinases, including VEGFR1, 2, and 3 (IC50s = 5, 1, and 3 nM, respectively).3 It also potently inhibits a variety of other receptor and non-receptor tyrosine kinases, including several in the platelet-derived growth factor, fibroblast growth factor, and endothelial growth factor receptor families.3,4 Cediranib blocks tubule formation by human umbilical vein endothelial cells in vitro and prevents angiogenesis as well as xenograft tumor growth in vivo.3 Because of these effects, cediranib has potential use in a range of cancers.5,6,7

1.Rini, B.I.Vascular endothelial growth factor-targeted therapy in metastatic renal cell carcinomaCancer115(10 Suppl)2306-2312(2009) 2.Burger, R.A.Overview of anti-angiogenic agents in development for ovarian cancerGynecol. Oncol.121(1)230-238(2011) 3.Wedge, S.R., Kendrew, J., Hennequin, L.F., et al.AZD2171: A highly potent, orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancerCancer Res.65(10)4389-4400(2005) 4.Davis, M.I., Hunt, J.P., Herrgard, S., et al.Comprehensive analysis of kinase inhibitor selectivityNat. Biotechnol.29(11)1046-1051(2011) 5.Bhargava, P., and Robinson, M.O.Development of second-generation VEGFR tyrosine kinase inhibitors: Current statusCurr. Oncol. Rep.13(2)103-111(2011) 6.Conti, A., Santoni, M., Amantini, C., et al.Progress of molecular targeted therapies for advanced renal cell carcinomaBiomed Res. Int.2013419176(2013) 7.Castelli, C., Tazzari, M., Negri, T., et al.Structured myeloid cells and anti-angiogenic therapy in alveolar soft part sarcomaJ. Transl. Med.11(1)237(2013)

实验参考方法

Kinase experiment:

The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFR-α, PDGFR-β, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aur-A, and Aur-B] using ELISA methodology[1].

Cell experiment:

Proliferation of MG63 osteosarcoma cells is induced by PDGF-AA, which selectively activates PDGFR-α homodimer signaling. 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 reincubated for 72 hours. Cellular proliferation is determined using a bromodeoxyuridine[1].

Animal experiment:

Rats: Young female Alderley Park rats (6 weeks of age, Wistar derived, n=5) are dosed orally, once daily for 28 days with Cediranib (1.25-5 mg per kg per day) or vehicle. Additional rats (five per group) are treated with Cediranib (5 mg per kg per day) or vehicle for 28 days and maintained for a further 28 days without treatment, to examine the effect of compound withdrawal. Histologic paraffin wax sections of the femorotibial joints and ovaries are stained with H&E. Morphometric image analysis of femorotibial sections is done, with growth plate areas from both the femur and tibia in each joint being combined for an analysis of the effect of compound treatment. The area of corpora lutea in H&E-stained ovary sections is similarly determined by morphometric analysis[1].

References:

[1]. Wedge SR, et al. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res, 2005, 65(10), 4389-4400.

化学性质

Cas No. 857036-77-2 SDF
别名 西地尼布马来酸盐; AZD-2171 maleate
Canonical SMILES O=C(O)/C=C\C(O)=O.FC1=C(OC2=C(C(C=C3OCCCN4CCCC4)=NC=N2)C=C3OC)C=CC5=C1C=C(C)N5
分子式 C29H31FN4O7 分子量 566.58
溶解度 DMSO : ≥ 45 mg/mL (79.42 mM);Water : 2 mg/mL (3.53 mM) 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.765 mL 8.8249 mL 17.6498 mL
5 mM 0.353 mL 1.765 mL 3.53 mL
10 mM 0.1765 mL 0.8825 mL 1.765 mL
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