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Rezivertinib
CAS No. 1835667-12-3
Rezivertinib ( —— )
产品货号. M34868 CAS No. 1835667-12-3
Rezivertinib (BPI-7711) 是一种口服有效，高选择性和不可逆的第三代 EGFR 酪氨酸激酶抑制剂 (TKI)。Rezivertinib 对常见的激活 EGFR 和抗性T790M 突变具有高效力。Rezivertinib 具有出色的透过中枢神经系统 (CNS) 能力，并具有抗肿瘤活性。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥550 | 有现货 |
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| 10MG | ￥905 | 有现货 |
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| 25MG | ￥1748 | 有现货 |
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| 50MG | ￥2948 | 有现货 |
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| 100MG | ￥4077 | 有现货 |
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| 200MG | ￥5742 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
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| 1G | 获取报价 | 有现货 |
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| 1 mL x 10 mM in DMSO | ￥587 | 有现货 |
|
生物学信息
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产品名称Rezivertinib
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述Rezivertinib (BPI-7711) 是一种口服有效，高选择性和不可逆的第三代 EGFR 酪氨酸激酶抑制剂 (TKI)。Rezivertinib 对常见的激活 EGFR 和抗性T790M 突变具有高效力。Rezivertinib 具有出色的透过中枢神经系统 (CNS) 能力，并具有抗肿瘤活性。
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产品描述Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
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体外实验Rezivertinib (BPI-7711) selectively inhibits cellular proliferation of EGFR mutations in cell lines: GI50 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), 22 nM (NCI-H1975, del19/T790M) and > 1000 nM (A431, EGFR WT).
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体内实验Rezivertinib (BPI-7711; 6.25-25 mg/kg/day; orally; 14 days) shows significant tumor regression.Rezivertinib (12.5 mg/kg/day; orally; 14 days) survives an average of 112% longer in H1975-luc human NSCLC mice model. Rezivertinib (50 mg/kg/day; orally) has anti-tumor efficacy correlated to improved average overall survival of the animals of 115% (28 days vs. 13 days).
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同义词——
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通路Angiogenesis
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靶点EGFR
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受体EGFR
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研究领域——
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适应症——
化学信息
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CAS Number1835667-12-3
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分子量486.57
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分子式C27H30N6O3
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO 中的溶解度 : 125 mg/mL (256.90 mM; 超声助溶 )
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SMILESO=C(C=C)NC1=CC(NC=2N=CC=C(N2)C3=CN(C=4C=CC=CC34)C)=C(OC)C=C1OCCN(C)C
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Misako Nagasaka, et al. Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC. J Thorac Oncol. 2021 May;16(5):740-763.?
