Phenylacetic acid mustard

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Phenylacetic acid mustard 

Phenylacetic acid mustard 是化疗试剂 Chlorambucil (HY-13593) 的主要代谢产物 (metabolite)。Chlorambucil 是一种烷化剂 (alkylator),具有抗肿瘤活性。

Phenylacetic acid mustard

Phenylacetic acid mustard Chemical Structure

CAS No. : 10477-72-2

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生物活性

Phenylacetic acid mustard is the major metabolite of the cancer chemotherapeutic agent Chlorambucil (HY-13593). Chlorambucil is an alkylating agent with antitumor activity[1].

IC50 & Target

IC50: metabolite of Chlorambucil[1]

体内研究
(In Vivo)

Phenylacetic acid mustard (intraperitoneal injection; 0-20 mg/kg; 15 days) shows consistently 1.8-1.9 times greater antitumour potency than CHL, it exhibits an ED15 value of 8.0 mg/kg[2].
Phenylacetic acid mustard (intraperitoneal injection; 0-20 mg/kg; single dose) cause 50% lethality at the dose 15.9 mg/kg[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Inbred male C3H/He mice[1]
Dosage: 0 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: Intraperitoneal injection; 15 days
Result: Exhibited anti-tumor activities in vivo.

分子量

276.16

Formula

C12H15Cl2NO2

CAS 号

10477-72-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
In Vivo:
  • 1.

    Phenylacetic acid mustard (PAAM) is dissolved in acidified ethanol (4.8 ml cone HC1 and 95% v/v ethyl alcohol in a volume of 100 ml) and diluted 1:9 with propylene glycol/K2HPO 4 buffer (20 g K2HPO4 plus 450 ml propylene glycol), final pH 7.4[2].

参考文献
  • [1]. Toni Pettersson-Fernholm, et al. Reactions of 4-bis(2-chloroethyl)aminophenylacetic acid (phenylacetic acid mustard) in physiological solutions.

    [2]. F Y Lee, et al. Pharmacokinetic basis for the comparative antitumour activity and toxicity of chlorambucil, phenylacetic acid mustard and, -difluorochlorambucil (CB 7103) in mice.

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