1. Protein Tyrosine Kinase/RTK
  2. FLT3 RET
  3. 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).

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PLM-101 Chemical Structure

PLM-101 Chemical Structure

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Description

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)[1].

In Vitro

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.

Molecular Weight

407.44

Formula

C22H22FN5O2

SMILES

FC1=CC2=C(C=C1)NC(/C2=C3NC4=CC=CC=C4C\3=N/OCCN5CCNCC5)=O

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
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PLM-101 Related Classifications

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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.

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Product Name:
PLM-101
Cat. No.:
HY-149539
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