2. Metabolic Enzyme/Protease Antibody-drug Conjugate/ADC Related
  3. ADC Cytotoxin Aminopeptidase
  4. 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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DTS-201 sodium Chemical Structure

DTS-201 sodium Chemical Structure

CAS No. : 372491-73-1

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DTS-201 sodium Related Antibodies

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Description

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[1].

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) is well tolerated in mice, rats, and dogs[1].
DTS-201 (i.v., 15 min, on day 1 and 22) 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) shows less cardiotoxicity than Doxorubicin[1].
DTS-201 (40-80 mg/kg, i.v.) has a better therapeutic index than free Doxorubicin in NCI-H1299, PC-3, and MDA-MB-231 xenograft mice[1].
Toxicokinetic variables of DTS-201in 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.

hERG IC50Dose (mg/kg) Dose (μmol/kg) Cmax (μM) Tmax (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
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.
Molecular Weight

1034.04

Formula

C49H64N5NaO18
CAS No.
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DTS-201 sodium Related Classifications

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  • 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:

DTS-201372491-73-1DTS201DTS 201ADC CytotoxinAminopeptidaseADC PayloadWBCMTDAntitumoralMDA-MB-231NCI-H1299Subchronic toxicityCardiac toxicityprostate cancerbreast cancerlung cancerInhibitorinhibitorinhibit

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