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BLU-945

CAS号

2660250-10-0

分子式

C28H37FN6O3S

主要靶点

EGFR

仅限科研使用

Cat No : CM11725

Print datasheet

Synonyms

BLU 945|BLU945|BLU-945|EGFR

验证数据展示

  • CAS No.: 2660250-10-0

    BLU-945
    CAS#: 2660250-10-0

产品信息

CAS号 2660250-10-0
分子式 C28H37FN6O3S
主要靶点 EGFR
主要通路 蛋白酪氨酸激酶|血管生成|JAK/STAT 信号通路
分子量 556.7
纯度 99.16%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 BLU 945|BLU945|BLU-945|EGFR

体内活性

方法：在携带NCI-H1975异种移植物的小鼠服用BLU-945（30，100 mg/kg ，每日二次）。 结果：100 mg / kg的BLU-945可以导致NCI-H1975异种移植物的小鼠体内肿瘤停滞。[1]

体外活性

BLU-945在 EGFR+/T790M 和 EGFR+/T790M/C797S 突变体中表现出亚纳摩尔活性，并保持对 EGFR 激活突变 (L858R、ex19del) 的活性，尤其是 EGFR L858R; BLU-945 对 pEGFR H1975 细胞系表现出优异的抑制活性 (IC50 = 1.1 nM)，其效力比 pEGFR A431（EGFR-WT 扩增细胞系）高出约 500 倍; 此外，BLU-945 可有效抑制 Ba/F3 工程细胞系中的 EGFR 磷酸化（L858R/T790M/C797S IC50= 3.2 nM，ex19del/T790M/C797S IC50 = 4.0 nM）[1]；BLU-945 (1-10000μM）可抑制 EGFR L858R/T790M/C797S 和 EGFR ex19del/T790M/C797S 突变细胞系中的 EGFR 磷酸化。[3]

溶解度

DMSO:100 mg/mL (179.6 mM)

参考文献

1.Eno MS, et al. Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer. J Med Chem. 2022 Jul 28;65(14):9662-9677.
2.John Emmerson Campbell, et al. Inhibitors of mutant forms of egfr. Patent WO2021133809A1.
3.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-small cell lung cancer.
4.Elaine Shum. et al. A phase 1/2 study of BLU-945 in patients with common activating EGFRmutant non-small cell lung cancer (NSCLC) (SYMPHONY trial-in-progress)

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
=
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×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2