R1530|882531-87-5|-陌孚医药/Medlife

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R1530

目录号: PL03672 纯度: ≥99%

CAS No. :882531-87-5

商品编号	规格	价格	会员价
PL03672-5mg	5mg	¥2250.00	请登录
PL03672-10mg	10mg	¥3375.00	请登录
PL03672-25mg	25mg	¥6750.00	请登录
PL03672-50mg	50mg	¥11733.00	请登录
PL03672-100mg	100mg	¥19287.00	请登录
PL03672-200mg	200mg	询价	询价
PL03672-500mg	500mg	询价	询价

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中文名称	R1530
中文别名	5-(2-氯苯基)-7-氟-1,2-二氢-8-甲氧基-3-甲基-吡唑并[3,4-b][1,4]苯并二氮杂卓;5-(2-氯苯基)-7-氟-1,2-二氢-8-甲氧基-3-甲基吡唑并[3,4-B][1,4]苯并二氮杂卓;R1530 抑制剂;5-(2-氯苯基)-7-氟-1,2-二氢-8-甲氧基-3-甲基吡唑并[3,4-b][1,4]苯并二氮杂卓
英文名称	R1530
英文别名	5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepine;CHEMBL1980391;R-1530;Kinome_3737;UNII-XQJ55R5PPQ;SureCN3824661;QC-10462;5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo(3,4-b)(1,4)benzodiazepine;Pyrazolo(3,4-b)(1,4)benzodiazepine, 5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl-;5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl-Pyrazolo[3,4-b][1,4]benzodiazepine;R 1530;R1530;5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl-pyrazolo[3,4-b][1,4]benzodiazepine
Cas No.	882531-87-5
分子式	C₁₈H₁₄ClFN₄O
分子量	356.78
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	R1530 是一种高效的，具有口服活性的有丝分裂/血管生成 (mitosis/angiogenesis) 双重作用抑制剂，具有抗肿瘤和抗血管生成活性。R1530 是一种多激酶抑制剂，与 31 种激酶结合的 K_d 均小于 500 nM。R1530 抑制 VGFr2、FGFr1 作用的 IC₅₀ 分别为 10 nM 和 28 nM。R1530 可以触发细胞凋亡 (有丝分裂) 或衰老。
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 K d values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC 50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence.
性状	Solid
IC50 & Target[1][2]	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). has not independently confirmed the accuracy of these methods. They are for reference only.
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
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]. Jin-Jun Liu, et al. Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors. ACS Med Chem Lett. 2013 Feb 14; 4(2): 259–263. [2]. Christian Tovar, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75.

溶解度数据	In Vitro: DMSO : 50 mg/mL (140.14 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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