(Z)-Orantinib|210644-62-5|((Z)-SU6668; (Z)-TSU-68)-陌孚医药/Medlife

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(Z)-Orantinib (Synonyms: (Z)-SU6668; (Z)-TSU-68)

目录号: PL09000 纯度: ≥99%

CAS No. :210644-62-5

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中文名称	(Z)-Orantinib
中文别名	抗癌医药中间体;(Z)-3-(2,4-二甲基-5-((2-氧代吲哚啉-3-亚基)甲基)-1H-吡咯-3-基)丙酸;5-[(Z)-(1,2-二氢-2-氧代-3H-吲哚-3-亚基)甲基]-2,4-二甲基-1H-吡咯-3-丙酸
英文名称	(Z)-Orantinib
英文别名	(Z)-3-(2,4-Dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid;(Z)-3-(2,4-Dimethyl-5-((2-oxoindolin-3-ylidene)-methyl)-1H-pyrrol-3-yl)propanoic acid;3-[2,4-dimethyl-5-(2-oxo-1,2-dihydroindol-3-ylidenemethyl)-1H-pyrrol-3-yl]propionic acid;PDGFR Tyrosine Kinase Inhibitor VI, SU6668;SU 6668;SU-6668;1H-Pyrrole-3-propanoic acid, 5-((1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-;1H-Pyrrole-3-propanoic acid, 5-[(Z)-(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-;3-(2,4-Dimethyl-5-((2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl)-1H-pyrrol-3-yl)propionic acid;3-(2,4-Dimethyl-5-(2-oxo-1,2-dihydroindol-3-ylidenemethyl)-1H-pyrrol-3-yl)propionic acid;Orantinib;SU6668;TSU 68;TSU68;9RL37ZZ665;2,4-Dimethyl-5-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-pyrrole-3-propanoic acid;3-(2,4-Dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid;Orantinibum;3-(2,4-dimethyl-5-{[(3Z)-2-oxo-1H-indol-3-ylidene]methyl}-1H-pyrrol-3-yl)propanoic acid;3-[2,4;(Z)-Orantinib
Cas No.	210644-62-5
分子式	C₁₈H₁₈N₂O₃
分子量	310.35
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	(Z)-Orantinib ((Z)-SU6668) 是一种有效，选择性，具有口服活性和 ATP 竞争性的 Flk‐1/KDR，PDGFRβ 和 FGFR1 抑制剂，IC₅₀ 值分别为 2.1，0.008 和 1.2 µM。(Z)-Orantinib 是有效的抗血管生成和抗肿瘤剂，可诱导已建立的肿瘤消退。
生物活性	(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC 50 s of 2.1, 0.008, and 1.2 μM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
性状	Solid
IC50 & Target[1][2]	Flk-1/KDR 2.1 μM (IC50) PDGFRβ 0.008 μM (I
体外研究(In Vitro)	SU6668 (5-15 min) inhibits Flk-1 trans-phosphorylation (Ki=2.1 μM), FGFR1 trans-phosphorylation (Ki=1.2 μM), and PDGFR autophosphorylation (Ki=0.008 μM). SU6668 (0.03-10 μM; 60 min) inhibits the VEGF-stimulated increase of KDR tyrosine phosphorylation in HUVECs. SU6668 inhibits mitogenesis of HUVECs induced by both VEGF and FGF in a dose-dependent manner with IC50s of 0.34 and 9.6 μM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	SU6668 (4-200 mg/kg/day; p.o. for 21 d) induces dose-dependent inhibition of A431 tumor growth in athymic mice. SU6668 (75 mg/kg/day; i.p. for 22 d) significantly suppresses tumor angiogenesis and vascularization in mice. SU6668 (200 mg/kg/day; p.o. for 11-27 d) induces striking regression of large established A431 xenografts in athymic mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Laird AD, et, al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60. [2]. Laird ad, et, al. SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice. FASEB J. 2002 May;16(7):681-90.

溶解度数据	In Vitro: DMSO : 50 mg/mL (161.11 mM; Need ultrasonic)配制储备液

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