SRX3207

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SRX3207 是具有口服活性的、首创的 Syk/PI3K 双抑制剂，其对 Syk 和 PI3Kα 的 IC50 值分别为 10.7 nM 和 861 nM。SRX3207 缓解抗肿瘤免疫抑制。

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.

SRX3207 (10 μmol/L) is able to block p-AKT at concentration.SRX3207 has sufficient solubility in water (43 μmol/L).

SRX3207 (10 mg/kg, orally) increases antitumor immune response.Animal Model:LLC or B16 or B16-OVA or CT26 (1 × 105) 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.

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PI3K/Akt/mTOR signaling

PI3K

PI3K | Syk

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2254693-15-5

555.65

C29H29N7O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 5 mg/mL (9.00 mM; 超声助溶 )

Cc1nn(cc1CN1CCC1)-c1ccnc(Nc2ccc(cc2)-c2csc3c2oc(cc3=O)N2CCOCC2)n1

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(-20℃)

With Ice Pack

≥ 2 years