SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression.
体外研究
SRX3207 (10 μmol/L) is able to block p-AKT at concentration.
SRX3207 has sufficient solubility in water (43 μmol/L).
LLC or B16 or B16-OVA or CT26 (1 × 10) cells were injected subcutaneously into syngeneic mice.
Dosage:
10 mg/kg.
Administration:
Orally, starting from day 10 when tumors reached 100 mm3 until tumors were harvested on day 21.
Result:
Blocked phosphorylation of Syk at 348 site and Y525/526 site.
Blocked immunosuppressive MΦ polarization.
Blocked tumor growth and increased survival effectively.
分子式
C29H29N7O3S
分子量
555.65
CAS号
2254693-15-5
运输条件
Room temperature in continental US; may vary elsewhere.