g5-7

JAK2 inhibitor G5-7 (JAK2 inhibitor G5-7) 是具有口服活性的JAK2变构抑制剂，可通过结合到 JAK2，选择性的抑制JAK2介导的 EGFR 和 STAT3 的磷酸化和激活。它诱导细胞周阻滞和诱导凋亡、具有抗血管生成活性。它有用于胶质瘤研究的潜能。

AMG 579 是一种有效的选择性 PDE10A 抑制剂 (IC50 = 0.1 nM)。

G-573 is an allosteric inhibitor of MEK that is both potent and selective. The IC(50) value for pERK inhibition in HCT116 tumours by G-573 was estimated to be 0.406  µM. The IC(50) values for tumour growth inhibition in HCT116 and H2122 were estimated to be 3.43 and 2.56 µM, respectively. ED(50) estimates in HCT116 and H2122 mouse xenograft models were estimated to be ~4.6 and 1.9 mg kg day, respectively.

Rozibafusp alfa为靶向ICOSLG的IgG2-κ型抗体，结合TNFSF13B融合蛋白。

G-5758 是一种具有口服有效性的IRE1α抑制剂，其对XBP1s的IC50为38 nM。G-5758 可应用于多发性骨髓瘤模型 (KMS-11) 的研究，大鼠在口服剂量高达500 mg kg时表现出良好的耐受性。G-5758 展示出与诱导IRE1敲低相当的药效学效果。