生物活性
R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence[1][2].
IC50 & Target
KDR
10 nM (IC50)
FGFR1
28 nM (IC50)
体外研究(In Vitro)
R1530 exhibits potent in vitro antiproliferative activity in all of the tumor cell lines ( IC50 = 0.2−3.4 μM)
R1530 inhibits the kinase activities of vascular endothelial growth factor receptor 2 (VGFr2), FGFr1 and PDGFr-β. R1530 has inhibition of VEGF and bFGF induces HUVEC proliferation ( IC50 = 49 and 118 nM)
体内研究
(In Vivo)
R1530 (1.56, 25, and 50 mg/kg; p.o.; daily, for 28 days.) has notable antitumor activity across a broad range of human xenograft models, with minimal toxicity[1].
Animal Model: Human tumor xenograft models[1]
Dosage: 1.56, 25 and 50 mg/kg
Administration: Oral administration; daily, for 28 days.
Result: Inhibited tumor growth in all models, with regression observed in all models tested at a 50 mg/kg dose.
分子量
356.78
性状
Solid
Formula
C18H14ClFN4O
CAS 号
882531-87-5
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : 50 mg/mL (140.14 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.8028 mL 14.0142 mL 28.0285 mL
5 mM 0.5606 mL 2.8028 mL 5.6057 mL
10 mM 0.2803 mL 1.4014 mL 2.8028 mL
*
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, 6 months; -20°C, 1 month。-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。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: