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. Mipsagargin is activated by PSMA-mediated cleavage of an inert masking peptide. Mipsagargin has the potential for refractory, advanced or metastatic solid tumours research.
| Molecular Weight | 1409.52 |
| Formula | C66H100N6O27 |
| CAS Number | 1245732-48-2 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Trine Bundgaard Andersen, et al. Molecules. Thapsigargin--from Thapsia L. to mipsagargin
[5] Nhu Thi Quynh Doan, et al. Steroids. Targeting thapsigargin towards tumors
| Related Drug-Linker Conjugates for ADC Products |
|---|
| SC-VC-PAB-MMAE
SC-VC-PAB-MMAE is part of a drug-linker conjugate for ADC (ADC) with anticancer activity, which consists of MMAE (a tubulin inhibitor) linked to a cleavable SC-VC-PAB linker. |
| DBCO-(PEG)3-VC-PAB-MMAE
DBCO-(PEG)3-vc-PAB-MMAE is an active molecule coupler (drug-linker conjugate for ADC) consisting of auristatin E attached to a DBCO-(PEG)3-vc-PAB connector. It can be used for cancer research. In addition, DBCO-(PEG)3-vc-PAB-MMAE is a click chemistry that contains a DBCO moiety and can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing an Azide moiety. |
| PB038
PB038 is a drug-liker containing a PEG unit and a cleavable linker attached to Exatecan. |
| Val-Ala-PAB-MMAE
Val-Ala-PAB-MMAE is a Drug-Linker Conjugate for ADC, consisting of ADC linker (Val-Ala-PAB) and MMAE. |
| Val-Ala-PABC-Exatecan
Val-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor). |
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