• All
  • Primary Antibodies
  • Conjugated Antibodies for IF
  • Conjugated Antibodies for FC
  • Secondary Antibodies
  • Antibody Labeling KitsNew
  • ELISA Kits
  • IHC Kits
  • Magnetic Cell Separation Kits
  • Cytokines & Growth Factors
  • Neutralizing/activating Antibodies
  • Nanobody-based Reagents
  • Accessory Products and Kits
  • Fusion Proteins
×
×
Host
0
Species Reactivity
0
Species Reactivity
0
Conjugate
0
Conjugate
0
Compatible Species
0
Conjugate
0

BLU-945

BLU-945 是一种强效的、高选择性的、口服有效的、可逆的表皮生长因子受体酪氨酸激酶抑制剂 (TKIs)。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。

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

BLU945|BLU 945

验证数据展示

  • CAS No.: 2660250-10-0

    BLU-945
    CAS#: 2660250-10-0

产品信息

BLU-945 is a potent, highly selective, reversible and orally active inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. 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).

CAS号 2660250-10-0
分子式 C28H37FN6O3S
主要靶点 EGFR
主要通路 JAK/STAT信号通路|蛋白酪氨酸激酶|血管生成
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 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 BLU945|BLU 945

体内活性

BLU-945 (oral, 0-100 mg/kg; bid) shows potent, robust EGFR pathway inhibition and anti-tumor activity in triple-mutant osimertinib-resistant Ba/F3 CDX and PDCX models[2].

体外活性

BLU-945 has inhibitory activity against the EGFRm/T790M double and EGFRm/T790M/C797Striple mutants, IC50 value range from 1.2-4.4 nM[2]. BLU-945 (0- 10 mM, 4 h) inhibit EGFR phosphorylation in the EGFR L858R/T790M/C797S, and EGFR ex19del/T790M/C797S mutant cell lines[2].

溶解度

DMSO:100 mg/mL (179.6 mM),ultrasonic and warming and heat to 60°C

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-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.
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 *
=
×
×

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