BLU-945 (Synonyms: ZL-2313)
目录号: PL04035 纯度: ≥99%
CAS No. :2660250-10-0
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中文名称
BLU-945
中文别名
蓝-945
英文名称
BLU-945
英文别名
BLU-945
Cas No.
2660250-10-0
分子式
C28H37FN6O3S
分子量
556.70
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
BLU-945 是一种强效、高选择性、可逆的表皮生长因子受体酪氨酸激酶抑制剂 (TKIs),具有口服活性。BLU-945 可有效抑制具有 L858R 和/或外显子 19 缺失突变、T790M 突变和 C797S 突变的 EGFR。BLU-945 可用于肺癌包括非小细胞肺癌(NSCLC)的研究。
生物活性
BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC).
性状
Solid
体外研究(In Vitro)
BLU-945 has inhibitory activity against the EGFRm/T790M double and EGFRm/T790M/C797Striple mutants with IC50 value range from 1.2-4.4 nM.
BLU-945 (0- 10 mM, 4 h) inhibit EGFR phosphorylation in the EGFR L858R/T790M/C797S, and EGFR ex19del/T790M/C797S mutant cell lines.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
BLU-945 (oral, 0-100 mg/kg; bid) demonstrates potent, robust EGFR pathway inhibition and anti-tumor activity in triple-mutant osimertinib-resistant Ba/F3 CDX and PDCX models. 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
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
ClinicalTrial
参考文献
[1]. John Emmerson Campbell, et al. Inhibitors of mutant forms of egfr. Patent WO2021133809A1.
[2]. Sun Min Lim, et al. BLU-945, a fourth-generation, potent and highly selective epidermal growth factor receptor tyrosine kinase inhibitor with intracranial activity, demonstrates robust in vivo anti-tumor activity in models of osimertinib-resistant non-sma
[3]. Meredith S Eno, et al. Discovery of BLU-94
溶解度数据
In Vitro: DMSO : 125 mg/mL (224.54 mM; ultrasonic and warming and heat to 60°C)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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