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

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.

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Antiproliferative agent-34

Antiproliferative agent-34 Chemical Structure

CAS No. : 2910858-34-1

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Antiproliferative agent-34 Related Antibodies

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Description

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]
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]
Molecular Weight

529.55

Formula

C27H27N7O5
CAS No.
SMILES

CN(C1=C2C=CC=C1)C=C2C3=NC(NC4=CC(OCCOCCN5C=CN=C5[N+]([O-])=O)=C(OC)C=C4)=NC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Antiproliferative agent-34 Related Classifications

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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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