2. Antibody-drug Conjugate/ADC Related
  3. Drug-Linker Conjugates for ADC
  4. Mipsagargin

Mipsagargin (G-202) 是一种基于毒胡萝卜素的新型靶向前体，由前列腺特异性膜抗原 (PSMA) 特异性肽与强效肌浆/内质网钙腺苷三磷酸酶 (SERCA) 泵抑制剂毒胡萝卜素 (HY-13433) 的类似物偶联而成。Mipsagargin 可以被 PSMA 介导的惰性掩蔽肽裂解激活。Mipsagargin 具有用于难治性、晚期或转移性实体瘤研究的潜力。

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Mipsagargin Chemical Structure

Mipsagargin Chemical Structure

CAS No. : 1245732-48-2

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Mipsagargin 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[1]

Traditional Cytotoxic Agents

 

体外研究
(In Vitro)

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 相关抗体:
体内研究
(In Vivo)

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.

Animal Model: MCF-7 human breast cancers growing in mice[1]
Dosage: 56 mg/kg
Administration: IV; 2 daily; 49 days
Result: Alone was able to produce significant (>50%) tumor regression.
This regression was stabilized when combined with daily dosing with the oral HDAC4 inhibitor, Tasquinimod (10 mg/kg/d; oral).
Animal Model: BALB/c mice[2]
Dosage: 67 mg/kg (Pharmacokinetic Analysis)
Administration: IV; a single dose
Result: Had a half-life of 4.9 hours.
Clinical Trial
分子量

1409.52

Formula

C66H100N6O27
CAS 号
Sequence

Asp-{Ggu}-{Ggu}-{Ggu}-{Ggu}
Sequence Shortening

D{Ggu}-{Ggu}-{Ggu}-{Ggu}
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Mipsagargin 相关分类

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Keywords:

Mipsagargin1245732-48-2G-202G202G 202Drug-Linker Conjugates for ADCThapsigarginprodrugPSMASERCA pumpthapsigargininert masking peptiderefractoryadvancedmetastatic solid tumoursInhibitorinhibitorinhibit

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目录号：
HY-16215
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