Tuspetinib, also known as HM43239, is an orally active small molecule inhibitor of FLT3 that selectively inhibits not only FLT3 wild type, ITD mutants or TKD mutations, but also FLT3 ITD/TKD double mutations. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1, known to be involved in tumor cell proliferation and/or differentiation HM43239 monotherapy induced dose-dependent regression of tumor growth in FLT3 wild-type and FLT3 mutated leukemia cancer cell line.
MedKoo Cat#: 207171
Name: Tuspetinib free base
CAS#: 2294874-49-8 (free base)
Chemical Formula: C29H33ClN6
Exact Mass: 500.2455
Molecular Weight: 501.08
Elemental Analysis: C, 69.51; H, 6.64; Cl, 7.07; N, 16.77
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 125.0 | 249.47 |
The following data is based on the product molecular weight 501.08 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 |
