Bioactivity | 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]. |
Invitro | PLM-101 (30 nM, 100 nM) 可抑制 PI3K 信号通路中 AKT (phospho-S473) 和 p70S6K (phospho-T389) 的磷酸化,以及 Ras 信号通路中 MEK (phospho-S217/S221) 和 ERK (phospho-T202/Y204) 的磷酸化[1]。 0 --> PLM-101 相关抗体: |
Name | PLM-101 |
Formula | C22H22FN5O2 |
Molar Mass | 407.44 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Choi YJ, et al. PLM-101 is a novel and potent FLT3/RET inhibitor with less adverse effects in the treatment of acute myeloid leukemia. Biomed Pharmacother. 2023 Sep;165:115066.. . |