Mipsagargin

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].

Product Specifications

CAS Number

[1245732-48-2]

Product Name Alternative

G-202

UNSPSC

12352209

Target

Calcium Channel; Peptide-Drug Conjugates (PDCs) ; PSMA

Type

Peptides

Related Pathways

Antibody-drug Conjugate/ADC Related; Immunology/Inflammation; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mipsagargin.html

Solubility

10 mM in DMSO

Smiles

CC1=C([C@@](OC2=O)([H])[C@]3([C@@]2(O)C)O)[C@]([C@](C)(C[C@@H]3OC(CCCCCCCCCCCNC(C[C@H](N)C(N[C@H](C(O)=O)CCC(N[C@H](C(O)=O)CCC(N[C@H](C(O)=O)CCC(N[C@H](C(O)=O)CCC(O)=O)=O)=O)=O)=O)=O)=O)OC(C)=O)([H])[C@H](OC(CCCCCCC)=O)[C@H]1OC(/C(C)=C\C)=O

Molecular Formula

C66H100N6O27

Molecular Weight

1409.52

References & Citations

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