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Phenformin HCl Sale

(Synonyms: 盐酸苯乙福明; Phenethylbiguanide hydrochloride) 目录号 : GC10461

An antihyperglycemic biguanide

Phenformin HCl Chemical Structure

Cas No.:834-28-6

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10g
¥368.00
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50g
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

BRAFV600E Me-1 melanoma cells and HEK-293 cells

Preparation method

The solubility of this compound in DMSO is > 12.1 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1 or 5 mM; 2 hrs

Applications

In BRAFV600E Me-1 melanoma cell line (with impaired AMPK activation), 1 and 5 mM Phenformin significantly increased AMPK kinase activity, in a dose-dependent manner. A similar increase was also observed in HEK-293 cells (as control cells). These results implied that the presence of BRAFV600E in melanoma cells did not prevent the pharmacological activation of AMPK, and that AMPK was activated by the increase in phosphorylation of a key AMPK downstream target (ACC).

Animal experiment [2]:

Animal models

Tyr::CreER; BRAFCA/+; PTENlox/lox mice bearing single tumor induced by 4-HT

Dosage form

100 mg/kg; p.o.; b.i.d.

Applications

In Tyr::CreER; BRAFCA/+; PTENlox/lox mice bearing single tumor induced by 4-HT, the combination of Phenformin and PLX4720 significantly inhibited tumor growth. PLX4720 alone substantially reduced the rate of tumor progression, but Phenformin alone only showed a modest inhibition on tumor growth in these mice. According to immunohistochemical analyses of these tumors, the Phenformin/PLX4720 combination dramatically promoted apoptotic cell death and inhibited tumor cell proliferation.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Petti C, Vegetti C, Molla A, Bersani I, Cleris L, Mustard KJ, Formelli F, Hardie GD, Sensi M, Anichini A. AMPK activators inhibit the proliferation of human melanomas bearing the activated MAPK pathway. Melanoma Res. 2012 Oct;22(5):341-50.

[2]. Yuan P, Ito K, Perez-Lorenzo R, Del Guzzo C, Lee JH, Shen CH, Bosenberg MW, McMahon M, Cantley LC, Zheng B. Phenformin enhances the therapeutic benefit of BRAF(V600E) inhibition in melanoma. Proc Natl Acad Sci U S A. 2013 Nov 5;110(45):18226-31.

产品描述

Phenformin hydrochloride is an anti-diabetic drug from the biguanide class, can activate AMPK activity.

Phenformin stimulates the phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering LKB1 activity[1]. Phenformin increases AMPK activity and phosphorylation in the isolated heart, the increase in AMPK activity is always preceded by and correlated with increased cytosolic [AMP][2]. Phenformin is a 50-fold more potent inhibitor of mitochondrial complex I than metformin. Phenformin robustly induces apoptosis in LKB1 deficient NSCLC cell lines. Phenformin at 2 mM similarly induces AMPK signaling as shown by increased P-AMPK and P-Raptor levels. Phenformin induces higher levels of cellular stress, triggering induction of P-Ser51 eIF2α and its downstream target CHOP, and markers of apoptosis at later times. Phenformin induces a significant increase in survival and therapeutic response in KLluc mice following long-term treatment[3]. Phenformin and AICAR increases AMPK activity in H441 cells in a dose-dependent fashion, stimulating the kinase maximally at 5-10 mm and 2 mm, respectively. Phenformin significantly decreases basal ion transport (measured as short circuit current) across H441 monolayers by approximately 50% compared with that of controls. Phenformin and AICAR significantly reduce amiloride-sensitive transepithelial Na+ transport compared with controls. Phenformin and AICAR suppress amiloride-sensitive Na+ transport across H441 cells via a pathway that includes activation of AMPK and inhibition of both apical Na+ entry through ENaC and basolateral Na+ extrusion via the Na+,K+-ATPase[4]. Phenformin-treated rats reveals a tendency towards a decrease in blood insulin level (radioimmunoassay)[5].

Phenformin increases levels of P-eIF2α and its target BiP/Grp78 in normal lung as well as in lung tumors of mice[3].

References:
[1]. Sakamoto K, et al. Activity of LKB1 and AMPK-related kinases in skeletal muscle: effects of contraction, phenformin, and AICAR. Am J Physiol Endocrinol Metab. 2004 Aug;287(2):E310-7.
[2]. Zhang L, et al. Metformin and phenformin activate AMP-activated protein kinase in the heart by increasing cytosolic AMP concentration. Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H457-66.
[3]. Moreira AL, et al. Thalidomide exerts its inhibitory action on tumor necrosis factor alpha by enhancing mRNA degradation. J Exp Med. 1993 Jun 1;177(6):1675-80.
[4]. Woollhead AM, et al. Phenformin and 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR) activation of AMP-activated protein kinase inhibits transepithelial Na+ transport across H441 lung cells. J Physiol. 2005 Aug 1;566(Pt 3):781-92. Epub 2005
[5]. Dilman VM, et al. Inhibition of DMBA-induced carcinogenesis by phenformin in the mammary gland of rats. Arch Geschwulstforsch. 1978;48(1):1-8.

Chemical Properties

Cas No. 834-28-6 SDF
别名 盐酸苯乙福明; Phenethylbiguanide hydrochloride
化学名 1-(diaminomethylidene)-2-(2-phenylethyl)guanidine;hydrochloride
Canonical SMILES C1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl
分子式 C10H16ClN5 分子量 241.72
溶解度 ≥ 12.1mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
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。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 4.137 mL 20.6851 mL 41.3702 mL
5 mM 0.8274 mL 4.137 mL 8.274 mL
10 mM 0.4137 mL 2.0685 mL 4.137 mL
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