Ilginatinib (NS018) is a potent and selective JAK2 inhibitor with potential therapeutic applications in myeloproliferative neoplasms (MPNs), particularly primary myelofibrosis (PMF). 1. Mechanism of Action: Ilginatinib specifically targets Janus kinase 2 (JAK2), including the mutant form JAK2V617F, which is commonly associated with MPNs. Compared to other JAK inhibitors, NS018 demonstrates high selectivity for JAK2 over JAK1, JAK3, and TYK2, reducing off-target effects. 2. Potency & IC50 Values: JAK2 IC50: Low nanomolar range (~1 nM in enzymatic assays). JAK2V617F Inhibition: Strong inhibition in cell-based assays, leading to reduced STAT5 phosphorylation. 3. Anti-Tumor Activity-Myelofibrosis Models: Demonstrates efficacy in preclinical mouse models by reducing splenomegaly, improving blood counts, and reversing bone marrow fibrosis. Cellular Effects: Inhibits proliferation of JAK2V617F-positive cell lines (e.g., SET-2) and suppresses JAK-STAT signaling.
MedKoo Cat#: 127531
Name: Ilginatinib HCl
CAS#: 1239358-85-0 (HCl)
Chemical Formula: C21H21ClFN7
Exact Mass: 0.0000
Molecular Weight: 425.90
Elemental Analysis: C, 59.22; H, 4.97; Cl, 8.32; F, 4.46; N, 23.02
The following data is based on the product molecular weight 425.90 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
