Lasmotinib

• Description :

  Lasmotinib (PHI-101) is a FLT3 and CHK2 inhibitor. Lasmotinib potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. Lasmotinib synergizes with Venetoclax (HY-15531) or Azacytidine to inhibit leukemia. Lasmotinib exhibits anticancer activity against ovarian and breast cancer[1][2][3][4].

• CAS Number :

  [2127107-15-5]

• Product Name Alternative :

  PHI-101

• UNSPSC :

  12352005

• Target :

  Checkpoint Kinase (Chk) ; FLT3

• Type :

  Reference compound

• Related Pathways :

  Cell Cycle/DNA Damage; Protein Tyrosine Kinase/RTK

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/phi-101.html

• Purity :

  98.97

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  NC(NC1=C(SC(C#CC2=CC(F)=CC=C2)=C1)C(N[C@H]3CCCNC3)=O)=O

• Molecular Formula :

  C19H19FN4O2S

• Molecular Weight :

  386.44

• References & Citations :

  [1]Nam K Y, et al. PHI-101 Is a Potent Third-Generation FLT3 Inhibitor Developed to Overcome Resistance in Acute Myeloid Leukemia[J]. Blood, 2020, 136: 28.|[2]Sung G J, Kim K A, Nam K Y, et al. Evaluation of Synergistic Anti-Leukemic Efficacy of PHI-101 in Preclinical Model of FLT3-ITD Acute Myeloid Leukemia. Blood, 2023, 142: 5949. |[3]Han J H J, Kim K T, Im J, et al. PHI-101, a potent and novel inhibitor of CHK2 in ovarian and breast cancer cells. Cancer Research, 2021, 81 (13_Supplement) : 1461-1461.|[4]Hwang H, Sung G J, Kim K A, et al. PHI-101 synergizes with chemotherapy and venetoclax in preclinical models of acute myeloid leukemia. Cancer Research, 2024, 84 (6_Supplement) : 7153-7153.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• Isoform :

  Chk2