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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- No. CAS: 2910858-34-1
- Fòrmula: C27H27N7O5
- Peso molecular:529.55
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Almacenamiento:
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Actividad biológica
Descripciòn
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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC827 | IC50 |
25 nM
Compound: A14
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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
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[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
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[PMID: 37356356] |
Chemical Information
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No. CAS 2910858-34-1
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Peso molecular 529.55
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Fòrmula C27H27N7O5
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SMILES
CN(C1=C2C=CC=C1)C=C2C3=NC(NC4=CC(OCCOCCN5C=CN=C5[N+]([O-])=O)=C(OC)C=C4)=NC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antiproliferative agent-34 Related Classifications
HY-155178 Related Classifications
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