R1530
更新时间：2026-02-07 18:07:41
采购访问：17次
| 常用名 | 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 | CAS号 | 882531-87-5 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities. IC50 Value: Target: VEGFR; PDGFRR1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. In addition, this agents exhibits anti-proliferative activity by initiating mitotic arrest and inducing apoptosis.in vitro: In the presence of R1530, polyploid cancer cells underwent apoptosis or became senescent which translated into potent in vitro and in vivo efficacy. Normal proliferating cells were resistant to R1530-induced polyploidy thus supporting the rationale for cancer therapy by induced polyploidy. Mitotic checkpoint kinase BubR1 was found downregulated during R1530-induced exit from mitosis, a likely consequence of PLK4 inhibition [1]. R1530 strongly inhibited human tumor cell proliferation. Growth factor-driven proliferation of endothelial and fibroblast cells was also inhibited [2].in vivo: Significant tumor growth inhibition was demonstrated in a lung cancer xenograft model with a range of once daily, weekly and twice-weekly doses of R1530 (3.125-50 mg/kg qd, 100 mg/kg qw, 100 mg/kg biw). Daily doses were most effective in the lung cancer model and also had significant growth inhibitory effects in models of colorectal, prostate, and breast tumors. Tumor regression occurred in all models treated with the maximum tolerated daily dose (50 mg/kg). The doses of 25 and 50 mg/kg qd resulted in biologically significant increased survival in all tested models. After oral administration in nude mice, R1530 showed good tissue penetration. Exposure was dose dependent up to 100 mg/kg with oral administration [2].Toxicity: N/AClinical trial: A Multiple Ascending Dose Study of R-1530 in Patients With Advanced Solid Tumors. Phase 1 物理化学性质： CAS号：882531-87-5 常用中文名：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 常用英文名：R1530 分子式：C18H14ClFN4O 分子量：356.781 密度：1.5±0.1 g/cm3 沸点：496.4±55.0 °C at 760 mmHg 熔点：N/A 闪点：254.0±31.5 °C 储存条件：2-8℃ |
上海念兴实业有限公司
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地区： 上海市 上海市 普陀区
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- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：R1530
- 价格： ￥645.9/10mg ￥2862.9/50mg ￥需询单/1g ￥需询单/1g
- 纯度：98.0%
- 备货期：1天
- 联系人：阿拉丁
- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：R1530
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
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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]苯并二氮杂卓生产厂家
参考价格：$138/10mM*1mLinDMSO