2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK) ROS Kinase
  4. ALK/ROS1-IN-1

ALK/ROS1-IN-1 (compound 2e) 是一种高效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂，对 ALK 和 ROS1 酶作用的 IC50 值分别为 0.174 μM 和 0.530 μM。

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ALK/ROS1-IN-1 Chemical Structure

ALK/ROS1-IN-1 Chemical Structure

CAS No. : 2365497-07-8

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ALK/ROS1-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

IC50 & Target

IC50: 0.174 μM (ALK), 0.530 μM (ROS1)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
3.64 μM
Compound: 2e
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31260890]
BaF3 IC50
104.7 nM
Compound: 2e
Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31260890]
BaF3 IC50
137.7 nM
Compound: 2e
Antiproliferative activity against mouse BAF3 cells expressing wild type CD74/ROS1 assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BAF3 cells expressing wild type CD74/ROS1 assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31260890]
BaF3 IC50
233.9 nM
Compound: 2e
Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 31260890]
HCC78 IC50
10.71 μM
Compound: 2e
Antiproliferative activity against ROS1-addicted human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against ROS1-addicted human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31260890]
NCI-H3122 IC50
6.45 μM
Compound: 2e
Antiproliferative activity against ALK-addicted human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against ALK-addicted human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31260890]
体外研究
(In Vitro)

ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC50= 6.27 μM and 10.71 μM, respectively)[1].
ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALKL1196M with an IC50 value of 41.3 nM[1].
ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC50s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively[1].
ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ALK/ROS1-IN-1 相关抗体:
分子量

584.63

Formula

C30H35F3N6O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ALK/ROS1-IN-1 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ALK/ROS1-IN-12365497-07-8Anaplastic lymphoma kinase (ALK)ROS KinaseAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246crizotinib-resistantALK/ROS1non-small-celllungcancerInhibitorinhibitorinhibit

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