Emavusertib 是一种IRAK4抑制剂，也是一种FLT3抑制剂，具有抗肿瘤作用。

Emavusertib is a potent IRAK4/FLT3 inhibtor. CA-4948 with anti-tumor activity.

CA-4948, demonstrated good cellular activity in ABC DLBCL and AML cell lines.?Inhibition of TLR signaling leading to decreased IL-6 levels was also observed in whole blood assays.?CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation.?CA-4948 was well tolerated in toxicity studies in both mouse and dog at efficacious exposure.?The overall profile of CA-4948 prompted us to select it as a clinical candidate for evaluation in patients with relapsed or refractory hematologic malignancies including non-Hodgkin lymphoma and acute myeloid leukemia[2].

1801344-14-8

C24H25N7O5

491.508

Emavusertib

DMSO:27.78 mg/mL (56.52 mM),Need ultrasonic
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years