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Art. -Nr.: HY-14833

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Atiratecan

(Synonyms: TP300)

Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models.

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CAS. Nr.: 867063-97-6
Formel: C₃₁H₃₄N₆O₆
Molecular Weight:586.64

Speicherung:

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

Data Sheet (279 KB)

Atiratecan Chemical Structure

CAS. Nr.: 867063-97-6

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Biologische Aktivität
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- In Vitro
- In Vivo
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Bioz

Biologische Aktivität

Beschreibung

Alle Topoisomerase Isoform-spezifische Produkte anzeigen :

In Vitro

Atiratecan (TP300) is stable in an acidic solution but is rapidly converted to CH0793076 under physiological pH conditions such as in sera^[1].
Atiratecan has antiproliferative activity against camptothecin-resistant cell lines. Atiratecan has IC₅₀s of 9.4 nM and 1.1 nM for A2780 and A2780/SN75 cells, respectively^[1].

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

In Vivo

Atiratecan (TP300; 47 mg/kg; IV; once per week for 3 weeks) shows more than 50% of tumor growth inhibition in all nine models, regardless of the expression of BCRP^[1].
Atiratecan (24 mg/kg; IV; once per week for 6 weeks) in combination with capecitabine results in synergistic eVects in the HCT116 human colon cancer and NCI-N87 human gastric cancer xenograft models and an additive eVect in the WiDr human colon cancer xenograft model which is BCRP-positive and CPT-11-insensitive^[1].
The eVective dose range of Atiratecan is between 0.30 and 47 mg/kg (MTD/ED₅₀=157). The toxic dose is 63 mg/kg for Atiratecan^[1].

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

Animal Model:

Five-week-old male athymic nude mice (CAnN.CgFoxn1^nu/CrlCrlj)^[1]
Dosage:

47 mg/kg (the maximum tolerated dose; MTD)
Administration:

IV; once per week for 3 weeks
Result:

Showed more than 50% of tumor growth inhibition in all models, regardless of the expression of BCRP.

Chemical Information

CAS. Nr. 867063-97-6
Molecular Weight 586.64
Formel C₃₁H₃₄N₆O₆
SMILES

O=C(O[C@](C(C=C12)=C(CO3)C(N1CC(C2=N4)=C5N(CCCCC)C=NC6=C5C4=CC=C6)=O)(CC)C3=O)CN(C(CN)=O)C
Synonyms

TP300
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 (279 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]. Endo M, et al. A water soluble prodrug of a novel camptothecin analog is efficacious against breast cancerresistance protein-expressing tumor xenografts. Cancer Chemother Pharmacol. 2010 Jan;65(2):363-71. [Content Brief]

Calculators

Molaritätsrechner

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

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.

MOQ

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100 mg

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Atiratecan

Alle Topoisomerase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

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Atiratecan Related Classifications

HY-14833 Related Classifications