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抑制剂/激活剂

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凋亡与自噬

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Semaxinib 司马沙尼; SU5416

Semaxinib (SU5416) 是有效，选择性的 VEGFR (Flk-1/KDR) 抑制剂，IC50 为 1.23 μM。

货号：
TK0430
规格：

5mg

10mg

50mg

100mg
价格：
￥0.00

产品参数

CAS No.	204005-46-9
生物活性	Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC50 of 1.23 μM.
分子式	C15H14N2O
分子量	238.28
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	DMF : 50 mg/mL (209.84 mM; Need ultrasonic) DMSO : 20 mg/mL (83.93 mM; Need ultrasonic)
体内研究	Daily administration of Semaxinib (SU5416) (i.p., 3 mg/kg/day) inhibits the local growth of C6 tumors in the colon. A comparable level of growth inhibition (62% by day 16; P=0.001) is observed for tumors growing in the colon in comparison with ones growing in the hindflank region (54% by day 18; P=0.001). These results indicate that Semaxinib (SU5416) could inhibit tumor growth at a site other than the subcutaneous implantation site, where the preexisting vasculature may be different. Daily treatment with Semaxinib (SU5416) (25 mg/kg) results in a significantly lower tumor growth rate with tumor masses of up to 8% of that present in control animals by day 22 after implantation. Inhibition of tumor growth is clearly preceded by a marked reduction of the tissue area covered by the newly formed glioma microvasculature in the Semaxinib-treated group, indicating a reduced initial tumor vascularization.
体外研究	Semaxinib (SU5416) inhibits VEGF-driven mitogenesis in a dose-dependent manner with an IC50 of 0.04±0.02 μM (n=3). In contrast, Semaxinib (SU5416) blocks FGF-dependent mitogenesis of HUVECs with an IC50 of 50 μM (n=10). An IC50 of 20.26±5.2 μM, which is about 20-fold less in potency on PDGF-dependent autophosphorylation, is observed when SU5416 is tested in NIH 3T3 cells overexpressing the human PDGF receptor β.
文献	•Adv Funct Mater. 2021 May 24. •Nat Commun. 2021 Oct 26;12(1):6177. •Hypertension. 2021 Sep 27;HYPERTENSIONAHA12016712. •Br J Pharmacol. 2021 Oct 2. •Am J Respir Cell Mol Biol. 2020 Jan;62(1):49-60. •Stem Cell Res Ther. 2021 May 10;12(1):281. •Transl Stroke Res. 2018 Oct;9(5):540-548. •Biomed Pharmacother. 2019 Dec;120:109491. •Antioxidants (Basel). 2018 Oct 26;7(11). pii: E150. •Acta Pharmacol Sin. 2021 Jan;42(1):108-114. •Front Cardiovasc Med. 2018 Aug 15;5:110. •Front Pharmacol. 2021 Nov 11;12:758763. •Front Pharmacol. 01 December 2021. •J Am Heart Assoc. 2019 Mar 5;8(5):e011227. •Cell Signal. 2018 Dec;52:147-154. •Am J Pathol. 2020 Jan;190(1):48-56. •Microvasc Res. 2022 Jan 4;104309. •Environ Toxicol Pharmacol. 2019 Apr 19;69:112-119. •Hypertens Res. 2020 Aug;43(8):754-764. •BMC Anesthesiol. 2019 Jul 9;19(1):127. •Transplant Proc. Jan-Feb 2020;52(1):419-422. •Physiol Rep. 2022 Jan;10(1):e15156. •Research Square Preprint. 2021 Oct. •Research Square Preprint. 2021 Feb.
纯度及产品资料	98%

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