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抑制剂/激活剂

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凋亡与自噬

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Pazopanib 帕唑帕尼; GW786034

Pazopanib (GW786034) 是多靶点抑制剂，抑制 VEGFR1，VEGFR2，VEGFR3，PDGFRβ，c-Kit，FGFR1，c-Fms的IC50分别为10，30，47，84，74，140，146 nM。

货号：
TK0546
规格：

2mg

5mg

10mg

25mg

50mg
价格：
￥0.00

产品参数

CAS No.	444731-52-6
生物活性	Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
分子式	C21H23N7O2S
分子量	437.52
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 50 mg/mL (114.28 mM; Need ultrasonic)
体内研究	Treatment of mice with 100 mg/kg of Pazopanib twice daily for five days results in significant inhibition in the degree of vascularization. The antiangiogenic activity of Pazopanib is examined in mice bearing established human xenografts (200−250 mm) using HT29 (colon carcinoma), A375P (melanoma), and HN5 (head and neck carcinoma) tumors following a standard three-week course of therapy. The HN5 and HT29 xenografts responded better at all doses compared to the A375P model, which is historically more resistant to VEGFR-2 inhibitors. As support that the observed inhibition of xenograft growth is working through an antiangiogenic rather than antitumor mechanism, no antiproliferative activity is observed below 10 μM for Pazopanib against these human tumor lines (HT29, HN5, A375P) growing in serum-containing media. No significant effect on the body weight of mice is observed, and the animals appeared healthy and active throughout the study duration. The quantity of adherent leukocytes in the Pazopanib eye drops group is less than untreated diabetic animals and more than the healthy animals. Average leukocytes adhered to the retinal vasculature in healthy animals is 37.2±7.8, whereas diabetic animals have an average value of 102±15.6, approximately 3-fold higher than healthy animals. Animals treated with 0.5 % w/v Pazopanib suspension demonstrate 69.5±9.5 leukocytes adhered in their retinal vasculature, which is found to be significantly lower than diabetic animals.
体外研究	Pazopanib shows good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity is also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, and c-fms with IC50s of 84, 74, 140, and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC50 of ~8 nM. Pazopanib possesses good pharmacokinetics in rat, dog, and monkey with low clearances (1.4-1.7 mL/min/kg) and good oral bioavailabilities (72, 47, 65%) dosed at 10, 1, and 5 mg/kg, respectively. The cytochrome P450 profile is also improved with inhibition >10 μM against the isozymes tested, with the exception of 2C9 (7.9 μM).
文献	•Cell Metab. 2021 Sep 8;S1550-4131(21)00375-2. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Cell Syst. 2018 Apr 25;6(4):424-443.e7. •Acta Pharmacol Sin. 2021 Jan;42(1):108-114. •J Cell Sci. 2015 Sep 1;128(17):3317-29. •ACS Chem Biol. 2017 May 19;12(5):1245-1256. •Exp Cell Res. 2020 Aug 1;393(1):112054. •J BUON. Jan-Feb 2020;25(1):464-471. •Patent. US20210299273A1. •Cell Physiol Biochem. 2016;38(3):926-38. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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