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Art. -Nr.: HY-P10759

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DTS-201 sodium

DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer.

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CAS. Nr.: 372491-73-1
Formel: C₄₉H₆₄N₅NaO₁₈
Molecular Weight:1034.04

Speicherung:

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

DTS-201 sodium Chemical Structure

CAS. Nr.: 372491-73-1

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Biologische Aktivität

Beschreibung

Alle Aminopeptidase Isoform-spezifische Produkte anzeigen :

CD13
LTA4H

In Vivo

DTS-201 (40-100 mg/kg in mice, 30-70 mg/kg in rats, and 4-8 mg/kg in dogs, i.v., 15 min) sodium is well tolerated in mice, rats, and dogs^[1].
DTS-201 (i.v., 15 min, on day 1 and 22) sodium is well tolerated in mice (50 mg/kg, MTD) and rats (40 mg/kg, MTD)^[1].
DTS-201 (3.2, 12.8 and 25.6 mg/kg, i.v., once weekly for 7 weeks) sodium shows less cardiotoxicity than Doxorubicin^[1].
DTS-201 (40-80 mg/kg, i.v.) sodium has a better therapeutic index than free Doxorubicin in NCI-H1299, PC-3, and MDA-MB-231 xenograft mice^[1].
Toxicokinetic variables of DTS-201 sodium in Beagle dogs after a 15-min intravenous infusion of DTS-201 at increasing dose levels

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

Animal Model:

Xenograft mouse models (seven-week-old male or female NMRI nu/nu mice were respectively injected with a PC-3 cell suspension (1 × 10⁷ cells/mL) or a MDA-MB-231 suspension (6 × 10⁷ cells/mL) in the ventral skin or implanted with a NCI-H1299 tumor fragment)^[1]
Dosage:

40 mg/kg, 60 mg/kg, 80 mg/kg
Administration:

Intraperitoneal injection (i.p.), weekly for 4 (NCI-H1299), 5 (PC-3), or 6 (MDA-MB-231) weeks
Result:

Showed to be more active at 40 mg/kg than Doxorubicin at the end of the study (PC-3 prostate cancer model).
Showed a higher activity in the MDA-MB-231 breast tumor model compared with Doxorubicin, with treated versus control values of 25% and 43%, respectively.
Showed significant dose-dependent efficacy, with treated versus control values of 38% and 17%, respectively in the NCI-H1299 lung cancer model.

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Chemical Information

CAS. Nr. 372491-73-1
Molecular Weight 1034.04
Formel C₄₉H₆₄N₅NaO₁₈
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)

Verweise

[1]. Ravel D, et al. Preclinical toxicity, toxicokinetics, and antitumoral efficacy studies of DTS-201, a tumor-selective peptidic prodrug of doxorubicin. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008, 14(4), 1258–1265. [Content Brief]

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Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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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Biologische Aktivität
- Beschreibung
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

hERG IC₅₀Dose (mg/kg)	Dose (μmol/kg)	C_max (μM)	T_max (min)	AUC_(0-t) (h ×μM)
4	3.9	14.4	15	5.1
8	7.8	42.6	15	15.7
16	15.5	83.6	15	38.2
32	31.0	209	15	127

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DTS-201 sodium

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