Denfivontinib, also known as G-749, is a novel, orally available FLT3 inhibitor. It selectively targets both FLT3 internal tandem duplication (ITD) and tyrosine kinase domain (TKD) mutations, including FLT3-D835, with nanomolar potency (IC₅₀ values typically <10 nM). Preclinical studies demonstrated that G-749 induces apoptosis and inhibits proliferation in FLT3-mutant AML cell lines and primary patient samples. It also showed strong anti-leukemic activity in FLT3-ITD xenograft mouse models, significantly reducing tumor burden and prolonging survival. Mechanistically, G-749 promotes degradation of FLT3 via disruption of chaperone protein interactions, in addition to kinase inhibition.
MedKoo Cat#: 406593
Name: Denfivontinib free base
CAS#: 1457983-28-6 (free base)
Chemical Formula: C25H25BrN6O2
Exact Mass: 520.1222
Molecular Weight: 521.41
Elemental Analysis: C, 57.59; H, 4.83; Br, 15.32; N, 16.12; O, 6.14
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 17.3 | 33.24 | |
| DMF | 16.0 | 30.69 | |
| DMF:PBS (pH 7.2) (1:3) | 0.3 | 0.48 |
The following data is based on the product molecular weight 521.41 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 |
