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Cat. No.: HY-128995

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Glycyl-Exatecan

Name: Glycyl-Exatecan
Brand: MedChemExpress
SKU: HY-128995
Availability: PreOrder

(Synonyms: Glycyl-DX-8951; Exatecan analog 2)

Glycyl-Exatecan (G-DX-8951) is a Topoisomerase I inhibitor. Glycyl-Exatecan exhibits weaker in vitro cytotoxicity than DX-8951 (HY-13631), and can further release DX-8951 in vivo. Glycyl-Exatecan can be used in studies related to Exatecan metabolism and antitumor drug delivery.

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

CAS No.: 849479-60-3
Formula: C₂₆H₂₅FN₄O₅
Molecular Weight:492.50

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (295 KB)

Glycyl-Exatecan Chemical Structure

CAS No.: 849479-60-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

Topoisomerase I

All Topoisomerase Isoforms :

In Vitro

Glycyl-Exatecan (G-DX-8951) exhibits almost comparable Topoisomerase I inhibitory activity to DX-8951 in preclinical in vitro studies, while its in vitro cytotoxicity is weaker than that of DX-8951^[1].

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

In Vivo

Glycyl-Exatecan (G-DX-8951) (6 mg/kg; i.v.; single dose) is released from DE-310 and distributed in plasma, tumor and liver after a single intravenous administration of DE-310 (5.7 mg DX-8951 equivalent/kg) to Meth A fibrosarcoma-bearing mice; Glycyl-Exatecan reaches the highest concentration at 24 h in tumor and 8 h in liver^[2].

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

Animal Model:

BALB/c (5-week-old; Meth A fibrosarcoma cells subcutaneously transplanted)^[2]
Dosage:

6 mg/kg
Administration:

i.v.; single dose
Result:

Reached maximum concentrations at 5 min in plasma, tumor, and liver; showed a tissue apparent terminal t_1/2 of 3.7-11 h and released DX-8951.

Chemical Information

CAS No. 849479-60-3
Molecular Weight 492.50
Formula C₂₆H₂₅FN₄O₅
SMILES

NCC(N[C@@H]1C2=C3C(C(N4C3)=CC([C@](O)(C(OC5)=O)CC)=C5C4=O)=NC6=CC(F)=C(C)C(CC1)=C62)=O
Synonyms

Glycyl-DX-8951; Exatecan analog 2
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (295 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wente MN, et al. DE-310, a macromolecular prodrug of the topoisomerase-I-inhibitor exatecan (DX-8951), in patients with operable solid tumors. Investigational new drugs. 2005 Aug;23(4):339-47. [Content Brief]

[2]. Masubuchi N. Pharmacokinetics of DE-310, a novel macromolecular carrier system for the camptothecin analog DX-8951f, in tumor-bearing mice. Pharmazie. 2004;59:374-377.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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