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

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Mipsagargin Chemical Structure

Mipsagargin Chemical Structure

CAS No. : 1245732-48-2

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Mipsagargin Related Antibodies

Top Publications Citing Use of Products

View All Drug-Linker Conjugates for ADC Isoform Specific Products:

View All Isoforms
Auristatin Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

 

In Vitro

Mipsagargin (G-202) is against the PSMA-nonproducing TSU cells (IC50=191 nM) and is 57-fold higher than that for the PSMA-producing LNCaP cells (IC50=5351 nM)[2].

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

Mipsagargin Related Antibodies
In Vivo

Mipsagargin (G-202; 56 mg/kg; 2 daily; 49 days) alone is able to produce significant (>50%) tumor regression. This regression is stabilized when combined with daily dosing with the oral HDAC4 inhibitor, Tasquinimod (HY-10528)[1].
Mipsagargin (56 mg/kg/day; for 3 consecutive days) produces ∼50% average regression of LNCaP xenografts in intact mice over a 30-day period. Significant antitumor effects are also observed against MDA-PCa2b and CWR22R-H out to ≥30 days after a single 3-day course of Mipsagargin[2].
Mipsagargin (67 mg/kg; IV) HaS a half-life of 4.9 hours in BALB/c mice[2].

MedChemExpress (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
Molecular Weight

1409.52

Formula

C66H100N6O27
CAS No.
Sequence

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

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Mipsagargin Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Mipsagargin
Cat. No.:
HY-16215
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.