2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Antiproliferative agent-34

Antiproliferative agent-34 (Compound A14) 是一种多靶点激酶抑制剂，对 EGFR L858R/T790M 和 EGFR WT 的 IC50 分别为 177 nM 和 1567 nM。Antiproliferative agent-34 还抑制 JAK2、ROS1、FLT3、FLT4、PDGFRα，IC50 为 30.93、106.90、108.00、226.60、42.53 nM。常氧条件下 Antiproliferative agent-34 抑制 H1975 和 HCC827 细胞增殖 的 IC50 值低于 40 nM，在缺氧条件下其抗增殖效力提高 4-6 倍 (IC50 值 < 10 nM)。

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Antiproliferative agent-34

Antiproliferative agent-34 Chemical Structure

CAS No. : 2910858-34-1

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Antiproliferative agent-34 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values < 10 nM) under hypoxic condition[1].

IC50 & Target

177, 30.93, 106.90, 108.00, 226.60, 42.53 nM for EGFR L858R/T790M, JAK2, ROS1, FLT3, FLT4, PDGFRα respectively[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCC827 IC50
25 nM
Compound: A14
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay
[PMID: 37356356]
HCC827 IC50
5.26 nM
Compound: A14
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay
Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay
[PMID: 37356356]
NCI-H1975 IC50
26.24 nM
Compound: A14
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under normoxia condition by SRB assay
[PMID: 37356356]
NCI-H1975 IC50
4.66 nM
Compound: A14
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs under hypoxia condition by SRB assay
[PMID: 37356356]
分子量

529.55

Formula

C27H27N7O5
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

Antiproliferative agent-34 相关分类

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  • 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:

Antiproliferative agent-342910858-34-1Antiproliferative agent34Antiproliferative agent 34EGFREpidermal growth factor receptorErbB-1HER1NSCLCH1975HCC827normoxichypoxicanti-proliferationInhibitorinhibitorinhibit

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