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Sardomozide dihydrochloride (CGP 48664A) Sale

(Synonyms: CGP 48664A) 目录号 : GC34074

An inhibitor of SAMDC

Sardomozide dihydrochloride (CGP 48664A) Chemical Structure

Cas No.:138794-73-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,914.00
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5mg
¥1,741.00
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10mg
¥3,169.00
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Sample solution is provided at 25 µL, 10mM.

Description

Sardomozide is an inhibitor of S-adenosylmethionine decarboxylase (SAMDC), an enzyme involved in polyamine biosynthesis (IC50 = 0.005 ?M for the rat liver enzyme).1 It is selective for SAMDC over diamine oxidase (DAO; IC50 = 18 ?M for the rat small intestine enzyme). Sardomozide inhibits the proliferation of T24 bladder cancer cells (IC50 = 0.71 ?M). It decreases intracellular levels of spermidine and spermine and increases intracellular putrescine levels in L1210 murine leukemia cells when used at a concentration of 3 ?M.2 Sardomozide (0.2 and 0.4 ?M) inhibits HIV-1 replication in PM1 cells.3 It reduces tumor growth in a SK-MEL-24 melanoma mouse xenograft model when administered at doses of 0.5 and 5 mg/kg.2

1.Stanek, J., Caravatti, G., Frei, J., et al.4-Amidinoindan-1-one 2'-amidinohydrazone: A new potent and selective inhibitor of S-Adenosylmethionine decarboxylaseJ. Med. Chem.36(15)2168-2171(1993) 2.Regenass, U., Mett, H., Stanek, J., et al.CGP 48664, a new S-adenosylmethionine decarboxylase inhibitor with broad spectrum antiproliferative and antitumor activityCancer Res.54(12)3210-3217(1994) 3.Sch?fer, B., Hauber, I., Bunk, A., et al.Inhibition of multidrug-resistant HIV-1 by interference with cellular S-adenosylmethionine decarboxylase activityJ. Infect. Dis.194(6)740-750(2006)

实验参考方法

Cell experiment:

The parent CHO cell line is chronically exposed to increasing levels of Sardomozide for at least eight passages beginning at 0.1 μM. Cell lines are serially exposed to increasing concentrations until a panel of sublines is obtained resistant to 1 (CHO/1). 3 (CHO/3), 10 (CHO/10), 30 (CHO/30), and 100 (CHO/100) μM Sardomozide for comparative studies[2].

References:

[1]. Regenass U, et al. CGP 48664, a new S-adenosylmethionine decarboxylase inhibitor with broad spectrum antiproliferative and antitumor activity. Cancer Res. 1994 Jun 15;54(12):3210-7.
[2]. Kramer DL, et al. Lysosomal sequestration of polyamine analogues in Chinese hamster ovary cells resistant to the S-adenosylmethionine decarboxylase inhibitor, CGP-48664. Cancer Res. 1998 Sep 1;58(17):3883-90.

化学性质

Cas No. 138794-73-7 SDF
别名 CGP 48664A
Canonical SMILES N=C(C1=CC=CC2=C1CC/C2=N\NC(N)=N)N.[H]Cl.[H]Cl
分子式 C11H16Cl2N6 分子量 303.19
溶解度 DMSO: 25 mg/mL (82.46 mM); Water: 10 mg/mL (32.98 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 3.2983 mL 16.4913 mL 32.9826 mL
5 mM 0.6597 mL 3.2983 mL 6.5965 mL
10 mM 0.3298 mL 1.6491 mL 3.2983 mL
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