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Home>>Signaling Pathways>>RSM-932A

RSM-932A Sale

(Synonyms: TCD-717) 目录号 : GC18847

RSM-932A 是一种 ChoKα 抑制剂，对多种肿瘤来源的细胞系具有有效的体外抗增殖活性，对小鼠的人异种移植物具有体内抗肿瘤活性。

RSM-932A Chemical Structure

Cas No.:850807-63-5

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1mg
¥361.00
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5mg
¥1,604.00
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10mg
¥2,663.00
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Sample solution is provided at 25 µL, 10mM.

GlpBio产品文献引用

产品描述 实验参考方法 化学性质 产品文档 相关产品

Description

RSM-932A is a ChoKα inhibitor with potent in vitro antiproliferative activity against a large variety of tumor-derived cell lines and in vivo antitumoral activity against human xenographs in mice. RSM-932A also shows high efficacy with low toxicity at the effective doses.[1]

In vitro experiments indicated that RSM-932A has a potent antiproliferative activity against most tumor-derived cell lines tested, including those derived from breast, lung, colon, bladder, liver, ovary, bone, cervix, kidney, pancreas, melanoma and brain tumors, with IC50 (1.15 ± 0.14 μM) in the low, single-digit micromolar range, consistent with a cytotoxic effect.

RSM-932A (72 h)

Type of tumor

Cell line

IC50

±SD

GI50

±SD

TGI

±SD

LC50

±SD

Breast 

MDA-MB-231 

1.3 

0.5 

1.2 

0.2 

2.0 

0.1 

2.7 

1.2 

T47D 

2,2 

0,9 

1,3 

0,8 

NA 

NA 

>6 

NA 

MDA.MB.468 

2.4 

1.0 

1.6 

0.4 

3.1 

1.6 

>6 

0.5 

SkBr-3 

3.1 

0.6 

1.0 

0.6 

1.6 

0.5 

13.2 

6.7 

Lung 

H510 

1.4 

0.3 

1.0 

NA 

1.1 

0.5 

3.9 

1.8 

H1299 

1.9 

0.1 

1.0 

0.0 

1.9 

0.7 

7.4 

3.0 

H460 

1.9 

0.5 

1.0 

0.0 

1.7 

0.6 

5.2 

1.3 

Colon 

HT-29 

1.7 

0.4 

1.3 

0.2 

5.6 

6.6 

11.0 

5.4 

HCT-116 

1.8 

0.3 

1.0 

0.3 

1.7 

1.0 

>6 

NA 

DLD-1 

2.1 

0.7 

1.6 

0.5 

3.3 

0.9 

6.3 

2.8 

SW620 

2.1 

0.7 

1.6 

0.5 

3.3 

0.9 

6.3 

2.8 

Bladder 

HT-1376 

1.5 

0.3 

1.0 

0.0 

5.7 

1.2 

>6.5 

NA 

TccSup 

1.6 

0.2 

1.1 

0.5 

1.5 

0.0 

>6.5 

NA 

SW780 

1.6 

0.4 

1.4 

0.3 

2.3 

0.5 

8.2 

3.1 

J82 

2.3 

1.3 

1.6 

1.2 

NA 

NA 

5.0 

2.1 

Epithelial carcinoma 

A431 

2.2 

0.1 

1.5 

0.5 

NA 

NA 

3.5 

0.7 

Liver 

Hep3B2 

2.4 

0.5 

1.2 

0.1 

2.7 

1.4 

3.2 

0.8 

HepG2 

6.4 

2.2 

1.3 

0.3 

8.4 

1.3 

>12 

NA 

Ovary 

OV-Car-3 

3.4 

0.3 

1.7 

0.2 

2.9 

0.4 

5.5 

0.5 

SK-OV-3 

6.4 

2.2 

1.3 

0.3 

8.4 

1.3 

>12 

NA 

Bone 

SAOS-2 

1.3 

0.1 

<1.6 

NA 

2.2 

0.7 

5.1 

1.5 

Cervix 

HeLa 

1.7 

0.7 

1.0 

NA 

1.5 

0.0 

5.7 

1.2 

Kidney 

769-P 

1.4 

0.2 

1.0 

0.4 

2.4 

1.2 

>3.5 

0.7 

Melanoma 

SKMel-28 

1.3 

0.3 

0.5 

0.0 

0.4 

0.1 

1.5 

0.4 

A-375 

6.2 

1.9 

2.6 

1.4 

5.6 

1.1 

7.7 

1.4 

Pancreas 

Mia.PaCa.2 

2.3 

0.2 

1.7 

0.3 

3.5 

0.4 

5.5 

1.4 

Astrocytoma, gliocystoma 

U-87 

1.9 

0.5 

1.4 

0.2 

5.0 

1.2 

8.9 

4.3 

Control 

MCF10-A 

7.1 

0.5 

3.4 

0.8 

7.2 

1.3 

14.7 

1.3 

Table 1.Panel of human cancer cell lines tested with RSM-932A for 72 hours and determination of IC50, GI50, TGI, and LC50 parameters

In vivo experiments demonstrated that RSM-932A shows no detectable toxicity in mice at highly effective doses with 77% tumor growth inhibition.[1]

References:
[1]. Lacal JC, et al. Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. Mol Cancer Ther. 2015 Jan;14(1):31-9.

\n\n\n\n\n\n

\n

RSM-932A 是一种 ChoKα 抑制剂，对多种肿瘤来源的细胞系具有有效的体外抗增殖活性，对小鼠的人异种移植物具有体内抗肿瘤活性。 RSM-932A 在有效剂量下也表现出高效低毒。[1]

体外实验表明，RSM-932A 对测试的大多数肿瘤衍生细胞系具有有效的抗增殖活性，包括来自乳腺、肺、结肠、膀胱、肝脏、卵巢、骨骼、子宫颈、肾脏、胰腺、黑色素瘤的细胞系和脑肿瘤，IC50 (1.15 ± 0.14 μM) 在低个位数微摩尔范围内，与细胞毒性作用一致。

\n<表格样式=\

实验参考方法

Cell experiment [1]:

Cell lines

DLD-1, HT29, SW620 and HCT116 CRC cell lines and the non-tumourigenic CCD-841 cell line

Preparation Method

6000 cells/well were seeded into 96- well flat-bottom plates and incubated for 24 h under standard conditions. MN58b or RSM-932A (TCD-717) were added at different concentrations from stocks solutions.

Reaction Conditions

2, 3, 4 µM, 24h

Applications

RSM-932A (TCD-717; 2-4 µM; for 24 hours) promotes cell death of colon cancer cells. ChoKα specific inhibitor RSM-932A (TCD-717), has demonstrated a potent antitumoral activity both in vitro and in vivo against several tumor-derived cell line xenografts including CRC-derived cell lines.
Animal experiment [2]:

Animal models

Six-week-old nude mice

Preparation Method

Mice were s.c. inoculated at lowers flanks with 1 × 106 of HT-29 cells suspended in 100μL of serum-free DMEM media mixed (1:1) with Matrigel. Measurable subcutaneous tumors (~0.15-0.2 cm3) were randomized to the treatment and control group. Tumor growth was monitored three times per week.

Dosage form

Effective dose of RSM-932A is 7.5 mg/kg, RSM-932A was dissolved at 50 mM 100% DMSO and administrated by i.v.. The successive dilutions were done fresh every day of treatment in sterile 5% dextrose water.

Applications

This could be used to perform growth inhibition studies at the specified effective dose. No significant organ damage was observed apart from hepatotoxicity that was found in all treatments except for the less aggressive treatment with RSM-932A that showed no liver toxicity while retaining a potent antitumoral activity.

References:

[1]. de la Cueva A, et al. Combined 5-FU and ChoKα inhibitors as a new alternative therapy of colorectal cancer: evidence in human tumor-derived cell lines and mouse xenografts. PLoS One. 2013 Jun 10;8(6):e64961.

[2]. Lacal JC, et al. Preclinical characterization of RSM-932A, a novel anticancer drug targeting the human choline kinase alpha, an enzyme involved in increased lipid metabolism of cancer cells. Mol Cancer Ther. 2015 Jan;14(1):31-9.

化学性质

Cas No. 850807-63-5 SDF
别名 TCD-717
化学名 1,1'-[[[1,1'-biphenyl]-4,4'-diyl]bis(methylene)]bis[4-[(4-chlorophenyl)methylamino]-quinolinium, dibromide
Canonical SMILES ClC1=CC=C(N(C2=CC=[N+](CC3=CC=C(C4=CC=C(C[N+]5=C(C=CC=C6)C6=C(N(C7=CC=C(Cl)C=C7)C)C=C5)C=C4)C=C3)C8=C2C=CC=C8)C)C=C1.[Br-].[Br-]
分子式 C46H38Cl2N4.2Br 分子量 877.5
溶解度 3mg/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 1.1396 mL 5.698 mL 11.396 mL
5 mM 0.2279 mL 1.1396 mL 2.2792 mL
10 mM 0.114 mL 0.5698 mL 1.1396 mL

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