PLM-101
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C22H22FN5O2
- Peso molecular:407.44
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-14 | GI50 |
23.1 nM
Compound: 9
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Antiproliferative activity against human MOLM-14 cells harboring FLT3 ITD/D835Y double mutant assessed as inhibition of cell growth incubated for 72 hrs by EZ-Cytox colorimetric assay
Antiproliferative activity against human MOLM-14 cells harboring FLT3 ITD/D835Y double mutant assessed as inhibition of cell growth incubated for 72 hrs by EZ-Cytox colorimetric assay
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[PMID: 35489222] |
| MOLM-14 | GI50 |
25.3 nM
Compound: 9
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Antiproliferative activity against human MOLM-14 cells assessed as inhibition of cell growth incubated for 72 hrs by EZ-Cytox colorimetric assay
Antiproliferative activity against human MOLM-14 cells assessed as inhibition of cell growth incubated for 72 hrs by EZ-Cytox colorimetric assay
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[PMID: 35489222] |
| MOLM-14 | GI50 |
75.6 nM
Compound: 9
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Antiproliferative activity against human MOLM-14 cells harboring FLT3 ITD/F691L double mutant assessed as inhibition of cell growth incubated for 72 hrs by EZ-Cytox colorimetric assay
Antiproliferative activity against human MOLM-14 cells harboring FLT3 ITD/F691L double mutant assessed as inhibition of cell growth incubated for 72 hrs by EZ-Cytox colorimetric assay
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[PMID: 35489222] |
| MV4-11 | GI50 |
3.69 nM
Compound: 9
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by EZ-Cytox colorimetric assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by EZ-Cytox colorimetric assay
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[PMID: 35489222] |
PLM-101 (30 nM, 100 nM) suppresses the phosphorylation of AKT (phospho-S473) and p70S6K (phospho-T389) in the PI3K signaling pathway, as well as the phosphorylation of MEK (phospho-S217/S221) and ERK (phospho-T202/Y204) in the Ras signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Peso molecular 407.44
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Fòrmula C22H22FN5O2
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SMILES
FC1=CC2=C(C=C1)NC(/C2=C3NC4=CC=CC=C4C\3=N/OCCN5CCNCC5)=O
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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)
PLM-101 Related Classifications
HY-149539 Related Classifications
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