Description
Atiratecan (TP300) is a prodrug 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.
Product information
CAS Number: 867063-97-6
Molecular Weight: 586.64
Formula: C31H34N6O6
Chemical Name: (10S)-10-ethyl-5,9-dioxo-23-pentyl-8-oxa-4,15,21,23-tetraazahexacyclo[14.7.1.0²,¹⁴.0⁴,¹³.0⁶,¹¹.0²⁰,²⁴]tetracosa-1,6(11),12,14,16,18,20(24),21-octaen-10-yl 2-(2-amino-N-methylacetamido)acetate
Smiles: CN(CC(=O)O[C@@]1(CC)C2C=C3C4=NC5=CC=CC6N=CN(CCCCC)C(C=65)=C4CN3C(=O)C=2COC1=O)C(=O)CN
InChiKey: CWJSAEZZZABNRI-HKBQPEDESA-N
InChi: InChI=1S/C31H34N6O6/c1-4-6-7-11-36-17-33-21-9-8-10-22-26(21)28(36)18-14-37-23(27(18)34-22)12-20-19(29(37)40)16-42-30(41)31(20,5-2)43-25(39)15-35(3)24(38)13-32/h8-10,12,17H,4-7,11,13-16,32H2,1-3H3/t31-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Atiratecan (TP300) is stable in an acidic solution but is rapidly converted to CH0793076 under physiological pH conditions such as in sera. 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.
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. 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. 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.
Products are for research use only. Not for human use.
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