Lasmotinib

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].

Product Specifications

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.