| Catalog No. | HC669086 |
|---|
| Species reactivity | Human |
|---|
| Applications | ELISA, Bioactivity: FACS, Functional assay, Research in vivo |
|---|
| Host species | Human |
|---|
| Isotype | IgG |
|---|
| Clone ID | MEDI3726 |
|---|
| Biological activity |
MEDI3726 (ADCT-401) exhibits potent, specific cytotoxicity in PSMA-expressing prostate cancer cell lines, with greatly reduced activity in PSMA-negative prostate cancer cell lines [3]. MEDI3726 (0.2 ug/mL; 1 h) cross-reacts with human and cynomolgus monkey soluble PSMA with similar potency, but does not cross-react with rat soluble PSMA [4]. MEDI3726 (up to 7 days) remains stable and active at 37°C in PBS, human plasma, or cynomolgus monkey plasma [4]. MEDI3726 (5-7 days) potently and specifically kills PSMA-positive human prostate cancer cell lines LNCaP (IC 50 = 0.02 nM), LNCaP C4-2 (IC 50 = 0.06 nM), MDA PCa 2b (IC 50 = 0.002 nM), and CWR22Rv1 (IC 50 = 0.29 nM), but shows no targeted cytotoxicity in PSMA-negative PC-3 (IC 50 = 29.3 nM) and DU145 cell lines (IC 50 = 44.9 nM) [4]. MEDI3726 (24 h) is specifically internalized and trafficked to lysosomes in PSMA-positive LNCaP cells, but not in PSMA-negative PC-3 cells [4]. MEDI3726 (6 nM; 2 h treatment) induces persistent DNA interstrand crosslinks in PSMA-positive LNCaP cells, but does not induce significant DNA crosslinking in PSMA-negative PC-3 cells [4]. catabolism primarily via heavy-light chain dissociation, with minimal warhead deconjugation. MEDI3726 can be used for the research of metastatic castration-resistant prostate cancer and prostate cancers [1] [2] [3] [4]. |
| Expression system |
Mammalian cells |
| Clonality |
Monoclonal |
| Target |
NAALAD1, Prostate-specific membrane antigen, NAALADase I, PSMA, PSM, Pteroylpoly-gamma-glutamate carboxypeptidase, Glutamate carboxypeptidase 2, N-acetylated-alpha-linked acidic dipeptidase I, Glutamate carboxypeptidase II, FOLH1, FGCP, FOLH, Folylpoly-gamma-glutamate carboxypeptidase, Folate hydrolase 1, GCPII, Membrane glutamate carboxypeptidase, Cell growth-inhibiting gene 27 protein, mGCP |
| Endotoxin level |
Please contact the lab for this information. |
| Purity |
>95% purity as determined by SDS-PAGE. |
| Purification |
Protein A/G purified from cell culture supernatant. |
| Accession |
Q04609 |
| Form |
Liquid |
| Storage buffer |
0.01M PBS pH 7.4 Please refer to the specific buffer information in the hardcopy of datasheet or the lot-specific COA.
|
| Stability and Storage |
Use a manual defrost freezer and avoid repeated freeze thaw cycles. Store at 2 to 8°C for frequent use. Store at -20 to -80°C for twelve months from the date of receipt. |
| Alternate Names | MEDI3726 |
|---|
| Background | Glutamate carboxypeptidase 2 (FOLH1/PSMA) is a ~84 kDa protein. Has both folate hydrolase and N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) activity. Has a preference for tri-alpha-glutamate peptides. In the intestine, required for the uptake of folate. In the brain, modulates excitatory neurotransmission through the hydrolysis of the neuropeptide, N-aceylaspartylglutamate (NAAG), thereby releasing glutamate. Involved in prostate tumor progression. |
|---|
| References |
1. de Bono JS, et al. Phase I Study of MEDI3726: A Prostate-Specific Membrane Antigen-Targeted Antibody-Drug Conjugate, in Patients with mCRPC after Failure of Abiraterone or Enzalutamide. Clin Cancer Res. 2021;27(13):3602-3609. [HC669086]
2. Huang Y, et al. Multifaceted Bioanalytical Methods for the Comprehensive Pharmacokinetic and Catabolic Assessment of MEDI3726, an Anti-Prostate-Specific Membrane Antigen Pyrrolobenzodiazepine Antibody-Drug Conjugate. Anal Chem. 2020;92(16):11135-11144. [HC669086]
3. Francesca Zammarchi, et al. ADCT-401/MEDI3726, a novel pyrrolobenzodiazepine (PBD)-based antibody-drug conjugate (ADC) targeting PSMA-expressing prostate cancers. Cancer Res 2017;77(13 Suppl):Abstract nr 3111A. [HC669086]
4. Cho S, et al. Antitumor Activity of MEDI3726 (ADCT-401), a Pyrrolobenzodiazepine Antibody-Drug Conjugate Targeting PSMA, in Preclinical Models of Prostate Cancer. Mol Cancer Ther. 2018;17(10):2176-2186. View More [HC669086] |
| Note |
For research use only. Not suitable for clinical or therapeutic use. |
中文
English
한국어
日本語
Español
Français
Русский
