9-Aminocamptothecin

Research use only, not for human use.

9-Aminocamptothecin is an inhibitor of topoisomerase I with potent anticancer activity.

9-Aminocamptothecin is an inhibitor of topoisomerase I with potent anticancer activity.(In Vitro):In human breast (MCF-7), bladder (MGH-U1), and colon (HT-29) cancer cell lines, 9-Aminocamptothecin cytotoxicity increases with both higher drug concentrations and longer exposure times. Minimal cell killing is also observed unless 9-Aminocamptothecin concentrations exceeds a threshold of 2.7 nm. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure.(In Vivo):9-Aminocamptothecin (9-Amino-CPT) inhibits tumor growth at the lowest oral dose (0.35 mg/kg/day), whereas higher oral doses (0.75 and 1 mg/kg/day) and s.c. administration (4 mg/kg/week) causes tumor regression. 9-Aminocamptothecin is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group. 9-Aminocamptothecin induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia. The oral and intravenous routes are equally effective. The results with this pre-clinical model support the evaluation of 9-Aminocamptothecin as antileukemic agent in a phase I trial in patients with AML.

In human breast (MCF-7), bladder (MGH-U1), and colon (HT-29) cancer cell lines, 9-Aminocamptothecin cytotoxicity increases with both higher drug concentrations and longer exposure times. Minimal cell killing is also observed unless 9-Aminocamptothecin concentrations exceeds a threshold of 2.7 nm. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure.

9-Aminocamptothecin (9-Amino-CPT) inhibits tumor growth at the lowest oral dose (0.35 mg/kg/day), whereas higher oral doses (0.75 and 1 mg/kg/day) and s.c. administration (4 mg/kg/week) causes tumor regression. 9-Aminocamptothecin is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group. 9-Aminocamptothecin induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia. The oral and intravenous routes are equally effective. The results with this pre-clinical model support the evaluation of 9-Aminocamptothecin as antileukemic agent in a phase I trial in patients with AML.

9-amino-CPT | 9-amino-2(S)-camptothecin | Aminocamptothecin

Cell Cycle/DNA Damage

Topoisomerase

Topo I

cancer

Ovarian Neoplasms

91421-43-1

363.4

C20H17N3O4

>98% (HPLC)

DMSO:3.33 mg/mL (9.16 mM)

CC[C@](C(C=C(c1nc2ccc3)N4Cc1cc2c3N)=C(CO1)C4=O)(C1=O)O

(S)-10-amino-4-ethyl-4-hydroxy-1H-pyrano[3'4':67]indolizino[12-b]quinoline-314(4H12H)-dione

(-20℃)

With Ice Pack

≥ 2 years