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PNU-159682

Catalog No. T16557 CAS 202350-68-3

PNU-159682 is a highly effective metabolite of the anthracycline nemorubicin. PNU-159682 has outstanding cytotoxicity. PNU-159682 is an effective ADCs cytotoxin.

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PNU-159682, CAS 202350-68-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 84.00
5 mg	In stock	$ 198.00
10 mg	In stock	$ 363.00
25 mg	In stock	$ 767.00
50 mg	In stock	$ 1,180.00
100 mg	In stock	$ 1,830.00

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Purity: 98.24%

Biological Description

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Description	PNU-159682 is a highly effective metabolite of the anthracycline nemorubicin. PNU-159682 has outstanding cytotoxicity. PNU-159682 is an effective ADCs cytotoxin.
Targets&IC50	CA IX:25 nM, Topo II unknotting activity:100 μM
In vitro	PNU-159682 inhibits a panel of human tumor cell lines (IC70 values in the range of 0.07-0.58 nM). PNU-159682 is 2,360- to 790-fold and 6,420- to 2,100-fold more potent than MMDX and doxorubicin, respectively. PNU-159682 displays cytotoxic effect on CAIX-expressing SKRC-52 cells (IC50: 25 nM). PNU-159682 (10 μM)-DNA adducts contain one or two drug molecules bound to double-stranded DNA. PNU-159682 (100 μM) weakly inhibits topoisomerase II unknotting activity [1][2][3].
In vivo	PNU-159682 (25 nmol/kg) shows an effective antitumor effect in mice bearing SKRC-52 xenografted tumors. PNU-159682 (15 μg/kg, i.v.) displays antitumor activity in mice bearing disseminated murine L1210 leukemia and in MX-1 human mammary carcinoma xenografts at 4 μg/kg[1][3].

Molecular Weight	641.62
Formula	C32H35NO13
CAS No.	202350-68-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 96.7 mg/mL (150.71 mM)

References and Literature

1. Quintieri L, et al. Formation and antitumor activity of PNU-159682, a major metabolite of nemorubicin in human liver microsomes. Clin Cancer Res. 2005 Feb 15;11(4):1608-17. 2. Cazzamalli S, et al. Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma. Mol Cancer Ther. 2016 Dec;15(12):2926-2935. 3. Scalabrin M, et al. Virtual Cross-Linking of the Active Nemorubicin Metabolite PNU-159682 to Double-Stranded DNA. Chem Res Toxicol. 2017 Feb 20;30(2):614-624.

Related Products

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Epirubicin hydrochloride Ciprofloxacin monohydrochloride Marbofloxacin Isodiospyrin Irinotecan hydrochloride trihydrate Alalevonadifloxacin Topoisomerase II inhibitor 14 Lauterine

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Keywords

PNU-159682 202350-68-3 DNA Damage/DNA Repair Topoisomerase PNU 159682 inhibit non-Hodgkin’s lymphoma PNU159682 ADCs Toxin acute myeloid leukemia ADC Payload EDV nanocell AML Inhibitor ADC Cytotoxin NMS249 NHL inhibitor

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