Hydroxy Camptothecine

Research use only, not for human use.

An alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata.

An alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme DNA topoisomerase, type I. Several semisynthetic analogs of camptothecin have demonstrated antitumor activity. (In Vitro):(±)-10-Hydroxycamptothecin (10-OH-camptothecin) is an inhibitor of topo I. (±)-10-Hydroxycamptothecin (10-HCPT, 5-20 nM) markedly inhibits the proliferation of Colo 205 cells in a dose-dependent manner. (±)-10-Hydroxycamptothecin (5-20 nM) arrests Colo 205 cells in the G2 phase of the cell cycle and triggers apoptosis through a caspase-3-dependent pathway. (±)-10-Hydroxycamptothecin (HPT, 0.01-10 μg/mL) causes cell shrinage, nuclear fragmentation and condensed chromosomes and induces apoptosis of human urinary bladder cancer cell line (T24).(In Vivo):(±)-10-Hydroxycamptothecin (10-HCPT, 2.5-7.5 mg/kg/2 days, p.o.) significantly suppresss tumor growth in mouse xenografts. (±)-10-Hydroxycamptothecin (1-7.5 mg/kg, p.o., once per 2 or 4 days) causes no obvious acute toxicity in nude mice.

(±)-10-Hydroxycamptothecin (10-OH-camptothecin) is an inhibitor of topo I. (±)-10-Hydroxycamptothecin (10-HCPT, 5-20 nM) markedly inhibits the proliferation of Colo 205 cells in a dose-dependent manner. (±)-10-Hydroxycamptothecin (5-20 nM) arrests Colo 205 cells in the G2 phase of the cell cycle and triggers apoptosis through a caspase-3-dependent pathway. (±)-10-Hydroxycamptothecin (HPT, 0.01-10 μg/mL) causes cell shrinage, nuclear fragmentation and condensed chromosomes and induces apoptosis of human urinary bladder cancer cell line (T24).

(±)-10-Hydroxycamptothecin (10-HCPT, 2.5-7.5 mg/kg/2 days, p.o.) significantly suppresss tumor growth in mouse xenografts. (±)-10-Hydroxycamptothecin (1-7.5 mg/kg, p.o., once per 2 or 4 days) causes no obvious acute toxicity in nude mice.

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Cell Cycle/DNA Damage

Topoisomerase

Topo I

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64439-81-2

364.35

C20H16N2O5

>98% (HPLC)

Soluble in DMSO

CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC(=CC5=C4)O)O

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(-20℃)

With Ice Pack

≥ 2 years