Mipsagargin  (Synonyms: G-202)

Mipsagargin (G-202) is a novel thapsigargin-based targeted proagent consisting of a prostate-specific membrane antigen (PSMA)-specific peptide coupled to an analog of the potent sarcoplasmic/endoplasmic reticulum calcium adenosine triphosphatase (SERCA) pump inhibitor Thapsigargin (HY-13433). Mipsagargin is activated by PSMA-mediated cleavage of an inert masking peptide. Mipsagargin has the potential for refractory, advanced or metastatic solid tumours research^[1][2][3].

Mipsagargin (G-202) 作用于不产生 PSMA 的 TSU 细胞 (IC₅₀=191 nM)，是产生 PSMA 的 LNCaP 细胞的 57 倍 (IC₅₀=5351 nM)^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Mipsagargin (G-202; 56 mg/kg; 静脉给药; 每天 2 次; 49 天) 单独能够产生显着的肿瘤消退 (>50%)。当同时每日服用口服 HDAC4 抑制剂 Tasquinimod (HY-10528) 时，这种趋势得到稳定^[1]。
Mipsagargin (56 mg/kg/天; 静脉给药; 连续 3 天) 在 30 天的时间内使完整小鼠的 LNCaP 异种移植物平均消退约 50%。在 Mipsagargin 的一个 3 天疗程后，针对 MDA-PCa2b 和 CWR22R-H 的显着抗肿瘤作用也观察到了长达 ≥ 30 天^[2]。
Mipsagargin (67 mg/kg; 静脉给药) 在 BALB/c 小鼠中的半衰期为 4.9 小时^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1409.52

C₆₆H₁₀₀N₆O₂₇

1245732-48-2

Asp-{Ggu}-{Ggu}-{Ggu}-{Ggu}

D{Ggu}-{Ggu}-{Ggu}-{Ggu}

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. John T Isaacs, et al. Mipsagargin: The Beginning-Not the End-of Thapsigargin Prodrug-Based Cancer Therapeutics. Molecules. 2021 Dec 9;26(24):7469.  [Content Brief]

  [2]. Samuel R Denmeade, et al. Engineering a prostate-specific membrane antigen-activated tumor endothelial cell prodrug for cancer therapy.  [Content Brief]

  [3]. D Mahalingam, et al. Mipsagargin, a novel thapsigargin-based PSMA-activated prodrug: results of a first-in-man phase I clinical trial in patients with refractory, advanced or metastatic solid tumours. Br J Cancer. 2016 Apr 26;114(9):986-94.  [Content Brief]