Irinotecan Hydrochloride Trihydrate - CAS 136572-09-3
Catalog number:
B0084-057943
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C33H38N4O6.HCl.3H2O
Molecular Weight:
677.18
COA:
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Targets:
Topoisomerase
Description:
The hydrochloride salt of Irinotecan. Irinotecan is a prodrug that can be activated to 7-ethyl-10-hydroxy-camptothecin (SN-38) by the carboxylesterase-converting enzyme. SN-38 inhibits topoisomerase I to suppress DNA replication and promote cell death.
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Catalog Number Size Price Stock Quantity
B0084-057943 1 g $198 In stock
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Brife Description:
topoisomerase I inhibitor
Purity:
>98%
Appearance:
Pale yellow to yellow crystalline solid
Synonyms:
CPT-11 HCl Trihydrate; Irinotecan Hcl Trihydrate; UNII-042LAQ1IIS
Solubility:
Soluble in DMSO
MSDS:
Inquire
Shelf Life:
2 years
Melting Point:
>245°C (dec.)
InChIKey:
KLEAIHJJLUAXIQ-JDRGBKBRSA-N
InChI:
InChI=1S/C33H38N4O6.ClH.3H2O/c1-3-22-23-16-21(43-32(40)36-14-10-20(11-15-36)35-12-6-5-7-13-35)8-9-27(23)34-29-24(22)18-37-28(29)17-26-25(30(37)38)19-42-31(39)33(26,41)4-2;;;;/h8-9,16-17,20,41H,3-7,10-15,18-19H2,1-2H3;1H;3*1H2/t33-;;;;/m0..../s1
Canonical SMILES:
CCC1=C2C=C(C=CC2=NC3=C1CN4C3=CC5=C(C4=O)COC(=O)C5(CC)O)OC(=O)N6CCC(CC6)N7CCCCC7.O.O.O.Cl
1.Establishment of a CPT-11-resistant human ovarian cancer cell line.
Kijima T1, Kubota N, Nishio K. Anticancer Res. 1994 May-Jun;14(3A):799-803.
A camptothecin analog, ((4s)-4,11-diethyl-4-hydroxy-9-[(4- piperidinopiperidino)carbonyloxy]dione hydrochloride trihydrate), (CPT-11), is a recently developed topoisomerase I (Topo I) inhibitor which attracts the attention of clinicians because of its high antitumor activity. We established a CPT-11-resistant human ovarian cell line, HAC2/CPT, from the parental HAC2 cell line. An in vitro drug sensitivity assay revealed that HAC2/CPT was 9.7 and 4.7 times as resistant as HAC2 to CPT-11 and 7-ethyl-10-hydroxy-CPT-11 (SN-38), an active metabolite of CPT-11, respectively. HAC2/CPT showed no cross-resistance to other drugs tested (adriamycin, etoposide, cisplatin and Taxol), suggesting that HAC2/CPT acquired a phenotype specifically resistant to the Topo I inhibitor. In order to elucidate the mechanism of the resistance, we measured Topo I activity of HAC2 and HAC2/CPT. The activity of Topo I of HAC2/CPT was reduced to half of that of the parental HAC2 cells.
2.Pharmacokinetics, metabolism, and excretion of irinotecan (CPT-11) following I.V. infusion of [(14)C]CPT-11 in cancer patients.
Slatter JG1, Schaaf LJ, Sams JP, Feenstra KL, Johnson MG, Bombardt PA, Cathcart KS, Verburg MT, Pearson LK, Compton LD, Miller LL, Baker DS, Pesheck CV, Lord RS 3rd. Drug Metab Dispos. 2000 Apr;28(4):423-33.
This study determined the disposition of irinotecan hydrochloride trihydrate (CPT-11) after i.v. infusion of 125 mg/m(2) (100 microCi) [(14)C]CPT-11 in eight patients with solid tumors. Mean +/- S.D. recovery of radioactivity in urine and feces was 95.8 +/- 2.7% (range 92.2-100.3%, n = 7) of dose. Radioactivity in blood, plasma, urine, and feces was determined for at least 168 h after dosing. Fecal excretion accounted for 63.7 +/- 6.8 (range 54.2-74.9%, n = 7) of dose, whereas urinary excretion accounted for 32.1 +/- 6.9% (range 21.7-43.8%; n = 7) of dose. One patient with a biliary T-tube excreted 30.1% of dose in bile, 14.2% in feces, and 48.2% in urine. Quantitative radiometric HPLC revealed that CPT-11 was the major excretion product in urine, bile, and feces. Aminopentane carboxylic acid (APC) and SN-38 glucuronide (SN-38G) were the most significant metabolites in urine and bile, whereas SN-38 and NPC, a primary amine metabolite, were relatively minor excretion products.
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CAS 136572-09-3 Irinotecan Hydrochloride Trihydrate

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