标签归档：atm

Mirin

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Mirin  纯度: 98.02%

Mirin 一种有效的 Mre11-Rad50-Nbs1 (MRN) 复合物抑制剂。Mirin 在不影响 ATM 蛋白激酶活性的情况下阻止 ATM (ataxia-telangiectasia mutated) 的 MRN 依赖性激活 (IC50=12 μM)，并抑制 Mre11 相关的核酸外切酶活性。Mirin 可消除哺乳动物细胞中的 G2/M 检查点和同源性依赖性修复。Mirin 在哺乳动物细胞中阻止 ATM 因 DNA 双链断裂 (DSBs) 而激活并阻断同源性定向修复 (HDR)。

Mirin

Mirin Chemical Structure

CAS No. : 299953-00-7

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Mirin 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library

生物活性

Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells[1].

体外研究
(In Vitro)

Mirin inhibits H2AX phosphorylation with an IC50 of 66 μM. Mirin also inhibits the ATM-dependent phosphorylation of the downstream targets Nbs1 and Chk2 and the MRN-dependent autophosphorylation of ATM at Ser1981 in response to DSBs. Mirin induces a substantial G2 arrest at concentrations of 50 μM and 100 μM. Mirin (10-100 μM) inhibits homology-dependent DNA repair in TOSA4 cells[1].
BRCA2-deficient cells also showed hypersensitivity to the Mre11 inhibitor Mirin[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

220.25

Formula

C10H8N2O2S
CAS 号

299953-00-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (378.34 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.5403 mL 22.7015 mL 45.4030 mL
5 mM 0.9081 mL 4.5403 mL 9.0806 mL
10 mM 0.4540 mL 2.2701 mL 4.5403 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。
参考文献

  • [1]. Dupré A, et al. A forward chemical genetic screen reveals an inhibitor of the Mre11-Rad50-Nbs1 complex. Nat Chem Biol. 2008;4(2):119-125.

    [2]. Ying S, et al. Mre11-dependent degradation of stalled DNA replication forks is prevented by BRCA2 and PARP1. Cancer Res. 2012;72(11):2814-2821.

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ATM-3507

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM-3507 

ATM-3507 是原肌球蛋白 (tropomyosin) 的一个有效抑制剂，其在人类黑色素瘤细胞系中的 IC50 值约为 3.83-6.84 μM。

ATM-3507

ATM-3507 Chemical Structure

CAS No. : 1861449-70-8

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ATM-3507 的其他形式现货产品:

ATM-3507 trihydrochloride

生物活性

ATM-3507 is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.

IC50 & Target

IC50: 3.83-6.84 μM (tropomyosin, in human melanoma celllines)[1].
体外研究
(In Vitro)

The cell lines differ in their relative expression of Tpm3.1 as well as in the expression of other isoforms. After determing the IC50 concentrations for TR100 and ATM-3507 (CHLA-20: 4.99±0.45 μM, CHP-134: 3.83±0.67 μM, CHLA-90: 6.84±2.37 μM, SK-N-BE(2): 5.00±0.42 μM) in each of the neuroblastoma cell lines, combinations of tropomyosin inhibitors plus Vincristine are tested at levels of each drug alone that kill less than 50% of the neuroblastoma cells. The combinations of both tropomyosin inhibitors plus Vincristine are completely cytotoxic in CHLA-20 cells. All 4 cell lines show some degree of synergy as determined by the Chou–Talalay method. The effect is not limited to the vinca alkaloids as a similar combination efficacy using paclitaxel plus TR100 or ATM-3507[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

The maximal tolerance dose (MTD) for TR100 and ATM-3507 is 60 and 150 mg/kg, respectively. It is found that a significant inhibition of tumor growth and prolongation of animal survival using either combination compared with each monotherapy. The median survival of mice increased from 18 days for mice treated with ATM-3507 to more than 49 days for mice treated with the combination. It is also found that twice weekly intravenous administration of ATM-3507 also show combination efficacy. The impact of each treatment or the combination on body weight is minimal. Drug levels are measured following the intravenous administration of ATM-3507 at 30 mg/kg in Balb/c mice (n=3 per time point). The mean half-life of ATM-3507 is 5.01 hrs for the terminal elimination phase. The mean AUC0-t in the plasma is 14,548 ng/h/mL. The Cmax of ATM-3507 is 5,758 ng/mL and the the t1/2 is 5.01 h. The observed plasma clearance and volume of distribution at steady state of ATM-3507 is 33.8 mL/min/kg and 7.23 L/kg, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

611.79

Formula

C37H46FN5O2
CAS 号

1861449-70-8
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.
参考文献

  • [1]. Currier MA, et al. Identification of Cancer-Targeted Tropomyosin Inhibitors and Their Synergy with Microtubule Drugs.Mol Cancer Ther. 2017 Aug;16(8):1555-1565.
Cell Assay
[1]

The 4 melanoma cell lines CHLA-20, CHLA-90, SK-N-BE(2) and CHP-134 are cultured at 37°C in a humidified incubator at 5% CO2 and supplemented 100 U/mL penicillin and 100 mg/mL streptomycin. Cells are plated in 96-well plates at 2000-4000 cells per well, incubated at 37°C overnight and then treated with various concentrations of TR100/ATM-3507 (0.1-2.5 μM) alone, TR100 and ATM-3507 plus various chemotherapy drugs. The cell viability is performed on day 3-5. For the dosing schedule optimization experiment, TR100 or Vincristine is added at day 1 with the other being added at day 2 or both TR100 and Vincristine are added on day 1 and plates are read at day 5. Results are presented as percentage of survival cells compared with controls. All cell viability assays are run in quadruplicate and the data shown are representative of at least 2 independent experiments[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Female athymic nude mice (age 4-6 weeks) are used. Mice are subcutaneously injected with 5.0×106 CHLA-20 cells in a 150 mL mix of PBS and Matrigel (2:1). ATM-3507 and TR100 are formulated at 15 mg/mL in 30% sulfobutyl-ether-b-cyclodextrin sodium salt (SBECD). Vincristine is dissolved in H2O at 0.125 mg/kg. When the tumors reached volumes of 200-400 mm3, mice are randomized into the study groups. Animals are followed until the animal reached endpoint criteria. Tumor size is measured using digital calipers twice per week and tumor volume is calculated. Mice are also weighed and observed twice per week for signs of endpoint condition. Mice that demonstrate signs of toxicity or reach endpoint criteria are humanely euthanized by CO2 as phyxiation and subjected to cervical dislocation as the secondary method of euthanasia[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Currier MA, et al. Identification of Cancer-Targeted Tropomyosin Inhibitors and Their Synergy with Microtubule Drugs.Mol Cancer Ther. 2017 Aug;16(8):1555-1565.

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ATM Inhibitor-2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM Inhibitor-2 

ATM Inhibitor -2 (化合物 7) 是一种强效的选择性 ATM 抑制剂，其 IC50 为 <1 nM。

ATM Inhibitor-2

ATM Inhibitor-2 Chemical Structure

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生物活性

ATM Inhibitor-2 (compound 7) is a potent and selective ATM inhibitor, with an IC50 of <1 nm[1].

IC50 & Target

ATM

<1 nM (IC50)

分子量

489.57

Formula

C26H31N7O3
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.
参考文献

  • [1]. Dimitrov T, et al. Development of novel urea-based ATM kinase inhibitors with subnanomolar cellular potency and high kinome selectivity. Eur J Med Chem. 2022 May 5;235:114234.

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ATM Inhibitor-3

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM Inhibitor-3 

ATM Inhibitor -3 (化合物 34) 是一种强效的选择性 ATM 抑制剂，其 IC50 为 0.71 nM。ATM Inhibitor-3 对 PI3K 激酶家族有抑制作用。ATM Inhibitor-3 具有良好的代谢稳定性。

ATM Inhibitor-3

ATM Inhibitor-3 Chemical Structure

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生物活性

ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability[1].

IC50 & Target

ATM

0.71 nM (IC50)

PI3K

 

mTOR

 

分子量

480.53

Formula

C25H29FN6O3
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.
参考文献

  • [1]. Dimitrov T, et al. Development of novel urea-based ATM kinase inhibitors with subnanomolar cellular potency and high kinome selectivity. Eur J Med Chem. 2022 May 5;235:114234.

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ATM Inhibitor-4

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM Inhibitor-4 

ATM Inhibitor -4 (化合物 39) 是一种强效的选择性 ATM 抑制剂，其 IC50 为 0.32 nM。ATM Inhibitor-4 对 PI3K 激酶家族有较强的抑制作用。ATM Inhibitor-4 在 1 μM 时能完全抑制 mTOR。ATM Inhibitor-4 具有良好的代谢稳定性。

ATM Inhibitor-4

ATM Inhibitor-4 Chemical Structure

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生物活性

ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability[1].

IC50 & Target

ATM

0.32 nM (IC50)

PI3K

 

mTOR

 

分子量

492.55

Formula

C26H29FN6O3
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.
参考文献

  • [1]. Dimitrov T, et al. Development of novel urea-based ATM kinase inhibitors with subnanomolar cellular potency and high kinome selectivity. Eur J Med Chem. 2022 May 5;235:114234.

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ATM-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM-IN-1 

ATM-IN-1 是一种有效的 ATM 抑制剂。ATM 主要位于细胞核和微粒体中，参与细胞周期进程和细胞周期检查点对 DNA 损伤的反应。ATM-IN-1 具有研究癌症和神经疾病的潜力 (摘自专利 WO2021139814A1，化合物 3)。

ATM-IN-1

ATM-IN-1 Chemical Structure

CAS No. : 2662761-76-2

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生物活性

ATM-IN-1 is a potent inhibitor of ATM. ATM is located mainly in the nucleus and microsomes and is involved in cell cycle progression and in the cell cycle checkpoint response to DNA damage. ATM-IN-1 has the potential for the research of cancer and neurology diseases (extracted from patent WO2021139814A1, compound 3)[1].

分子量

528.65

Formula

C30H36N6O3
CAS 号

2662761-76-2
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.
参考文献

  • [1]. Wenyuan Qian, et al. Quinoline and imidazole compounds and their applications. Patent WO2021139814A1.

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ATM-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM-IN-1 

ATM-IN-1 是一种有效的 ATM 抑制剂。ATM 主要位于细胞核和微粒体中，参与细胞周期进程和细胞周期检查点对 DNA 损伤的反应。ATM-IN-1 具有研究癌症和神经疾病的潜力 (摘自专利 WO2021139814A1，化合物 3)。

ATM-IN-1

ATM-IN-1 Chemical Structure

CAS No. : 2662761-76-2

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生物活性

ATM-IN-1 is a potent inhibitor of ATM. ATM is located mainly in the nucleus and microsomes and is involved in cell cycle progression and in the cell cycle checkpoint response to DNA damage. ATM-IN-1 has the potential for the research of cancer and neurology diseases (extracted from patent WO2021139814A1, compound 3)[1].

分子量

528.65

Formula

C30H36N6O3
CAS 号

2662761-76-2
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.
参考文献

  • [1]. Wenyuan Qian, et al. Quinoline and imidazole compounds and their applications. Patent WO2021139814A1.

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ATM-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM-IN-1 

ATM-IN-1 是一种有效的 ATM 抑制剂。ATM 主要位于细胞核和微粒体中，参与细胞周期进程和细胞周期检查点对 DNA 损伤的反应。ATM-IN-1 具有研究癌症和神经疾病的潜力 (摘自专利 WO2021139814A1，化合物 3)。

ATM-IN-1

ATM-IN-1 Chemical Structure

CAS No. : 2662761-76-2

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生物活性

ATM-IN-1 is a potent inhibitor of ATM. ATM is located mainly in the nucleus and microsomes and is involved in cell cycle progression and in the cell cycle checkpoint response to DNA damage. ATM-IN-1 has the potential for the research of cancer and neurology diseases (extracted from patent WO2021139814A1, compound 3)[1].

分子量

528.65

Formula

C30H36N6O3
CAS 号

2662761-76-2
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.
参考文献

  • [1]. Wenyuan Qian, et al. Quinoline and imidazole compounds and their applications. Patent WO2021139814A1.

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ATM Inhibitor-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM Inhibitor-1 

ATM Inhibitor-1 是一种有效、选择性、可口服的 ATM 抑制剂，IC50 值为 0.7 nM，对 mTOR (IC50，21 μM)，DNAPK (IC50，2.8 μM)，PI3Kα (IC50，3.8 μM)，PI3Kβ (IC50，10.3 μM)，PI3Kγ (IC50，3 μM) 和 PI3Kδ (IC50，0.73 μM) 的作用很弱。ATM Inhibitor-1 具有抗肿瘤活性。

ATM Inhibitor-1

ATM Inhibitor-1 Chemical Structure

CAS No. : 2135639-94-8

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生物活性

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity[1].

IC50 & Target[1]

ATM

0.7 nM (IC50)

ATM

2.8 nM (IC50, Cellular assay)

mTOR

21 μM (IC50)

DNAPK

2.8 μM (IC50)

PI3Kα

3.8 μM (IC50)

PI3Kβ

10.3 μM (IC50)

PI3Kγ

3 μM (IC50)

PI3Kδ

0.73 μM (IC50)

体外研究
(In Vitro)

ATM Inhibitor-1 (Compound 21) is a highly potent, selective and orally active ATM Inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM)[1].
In cellular assays, ATM Inhibitor-1 exhibits IC50s of 2.8 nM, >30 μM and >19 μM for ATM, ATR/PI3Kα and PI3Kβ/mTOR, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

ATM Inhibitor-1 (Compound 21; 50 mg/kg p.o. once daily for 3 days every week starting 24 h post-irinotecan dosing, 21 days) in combination with 50 mg/kg irinotecan significantly reduces tumor growth in SW620 mice model[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SW620 mice model[1]
Dosage: 50 mg/kg
Administration: P.O., once daily for 3 days every week starting 24 h post-irinotecan dosing, 21 days
Result: Inhibited the growth of tumor combined with 50 mg/kg irinotecan in SW620 mice model.

分子量

492.61

Formula

C27H36N6O3
CAS 号

2135639-94-8
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.
参考文献

  • [1]. Barlaam B, et al. Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors. CS Med Chem Lett. 2018 Jul 13;9(8):809-814.

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AZD0156

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AZD0156  纯度: 99.62%

AZD0156 是一种有效的，选择性的和口服活性的 ATM 抑制剂，IC50 为 0.58 nM。AZD0156 抑制 ATM 介导的信号转导，防止 DNA 损伤检查点激活，破坏 DNA 损伤修复，并诱导肿瘤细胞凋亡 (apoptosis)。

AZD0156

AZD0156 Chemical Structure

CAS No. : 1821428-35-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥780 In-stock
10 mg ￥1300 In-stock
50 mg ￥4000 In-stock
100 mg ￥5600 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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  • Targeted Diversity Library

生物活性

AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis[1].

IC50 & Target[1]

ATM

 

体外研究
(In Vitro)

AZD0156 inhibits the kinase activity of ATM and ATM-mediated signaling, prevents DNA damage checkpoint activation, and disrupts DNA damage repair, inducs tumor cell apoptosis, and leads to cell death in ATM-overexpressing tumor cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

461.56

Formula

C26H31N5O3
CAS 号

1821428-35-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 20 mg/mL (43.33 mM; ultrasonic and adjust pH to 3 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1666 mL 10.8328 mL 21.6657 mL
5 mM 0.4333 mL 2.1666 mL 4.3331 mL
10 mM 0.2167 mL 1.0833 mL 2.1666 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 0.83 mg/mL (1.80 mM); Clear solution; Need ultrasonic

    此方案可获得 0.83 mg/mL (1.80 mM) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 0.83 mg/mL (1.80 mM); Suspended solution; Need ultrasonic

    此方案可获得 0.83 mg/mL (1.80 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: 0.83 mg/mL (1.80 mM); Clear solution; Need ultrasonic

    此方案可获得 0.83 mg/mL (1.80 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer.?
Cell Assay
[1]

HT29 cells are seeded into 384 well assay plates at a density of 6000 cells/well in 40 μL EMEM medium containing 1% L glutamine and 10% FBS and allowed to adhere overnight. The following morning compound of Formula (I) in 100% DMSO is added to assay plates by acoustic dispensing. After lh incubation at 37°C and 5% C02, 40 nL of 3 mM 4NQO in 100% DMSO is added to all wells by acoustic dispensing, except minimum control wells which are left untreated with 4NQO to generate a null response control. Plates are returned to the incubator for a further lh. Then cells are fixed by adding 20 μL of 3.7% formaldehyde in PBS solution and incubating for 20 mins at r.t.. Then 20 μL of 0.1% Triton XI 00 in PBS is added and incubated for 10 minutes at r.t., to permeabalise cells. Then the plates are washed once with 50 μL/well PBS, using a Biotek EL405 plate washer.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer.?

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

AZD1390

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AZD1390  纯度: 99.97%

AZD1390 是一种有效的，高度选择性的，口服生物利用的，可渗透脑的 ATM 抑制剂，在细胞中对 ATM 的 IC50 为 0.78 nM。

AZD1390

AZD1390 Chemical Structure

CAS No. : 2089288-03-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1839 In-stock
1 mg ￥990 In-stock
5 mg ￥1750 In-stock
10 mg ￥2800 In-stock
25 mg ￥5400 In-stock
50 mg ￥9900 In-stock
100 mg   询价  
200 mg   询价  

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  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library

生物活性

AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell[1].

IC50 & Target[1]

ATM

 

体内研究
(In Vivo)

Median survival of mice treated with AZD1390 and radiation are significantly longer than untreated control mice (p=0.001). No overt signs of treatment toxicity are observed with small animal radiation research platform (SARRP) contrary to wholehead irradiated mice that seem to develop mucositis and difficulties drinking and eating at doses >10 Gy in combination with AZD1390[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

477.57

Formula

C27H32FN5O2
CAS 号

2089288-03-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (52.35 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0939 mL 10.4697 mL 20.9393 mL
5 mM 0.4188 mL 2.0939 mL 4.1879 mL
10 mM 0.2094 mL 1.0470 mL 2.0939 mL

*

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, 6 months; -20°C, 1 month。-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。
参考文献

  • [1]. Durant ST, et al. The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models. Sci Adv. 2018 Jun 20;4(6):eaat1719.

    [2]. J. Kahn, et al. Next-Generation ATM Kinase Inhibitors Under Development Radiosensitize Glioblastoma With Conformal Radiation in a Mouse Orthotopic Model. IJROBP. 2017. 99, 600-601.
Animal Administration
[2]

Mouse GL261 glioma (p53 mutant) cells are implanted intra-cranially into immunocompetent, syngeneic C57/bl6 mice followed by bioluminescent imaging (BLI) prior to randomization. AZD1390 is administered by oral gavage prior to deliver multiple fractions of 2-3 Gy of radiation on 2 to 4 consecutive days. Radiation is administered via small animal radiation research platform (SARRP) irradiation to the site of the tumor with a 5×5 mm lateral field[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Durant ST, et al. The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models. Sci Adv. 2018 Jun 20;4(6):eaat1719.

    [2]. J. Kahn, et al. Next-Generation ATM Kinase Inhibitors Under Development Radiosensitize Glioblastoma With Conformal Radiation in a Mouse Orthotopic Model. IJROBP. 2017. 99, 600-601.

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AT7519 TFA(Synonyms: AT7519M TFA)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AT7519 TFA (Synonyms: AT7519M TFA) 纯度: 98.53%

AT7519 (AT7519M) TFA 是一种有效的 CDK 抑制剂，对 CDK1，CDK2，CDK4-CDK6 以及 CDK9 的 IC50 值分别为 210，47，100，13，170 和 <10 nM。

AT7519 TFA(Synonyms: AT7519M TFA)

AT7519 TFA Chemical Structure

CAS No. : 1431697-85-6

规格 价格 是否有货 数量
5 mg ￥810 In-stock
10 mg ￥1350 In-stock
50 mg ￥4450 In-stock
100 mg ￥6900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AT7519 TFA 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
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  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
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  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

AT7519 (AT7519M) TFA as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

IC50 & Target[2]

CDK9/Cyclin T

10 nM (IC50)

CDK5/p35

13 nM (IC50)

cdk2/cyclin A

47 nM (IC50)

Cdk4/cyclin D1

100 nM (IC50)

cdk6/cyclin D3

170 nM (IC50)

Cdk1/cyclin B

210 nM (IC50)

CDK7/Cyclin H/MAT1

2400 nM (IC50)

GSK3β

89 nM (IC50)

体外研究
(In Vitro)

AT7519 (0-4 μM) TFA results in dose-dependent cytotoxicity with IC50s ranging from 0.5 to 2 μM in MM cells, and this induced cytotoxicity is associated with GSK-3β activation independent of transcriptional inhibition. AT7519 TFA overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) TFA induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) TFA inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells[1]. AT7519 (250 nM) TFA inhibits cell cycle progression in human tumor cell lines. AT7519 TFA also induces apoptosis of human tumor cell lines[2]. AT7519 (100-700 nM) TFA induces apoptosis in leukemia cell lines. AT7519TFA also inhibits transcription in human tumor cell lines. Furthermore, AT7519 TFA inhibits RNA polymerase II and reduces antiapoptotic protein levels[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

AT7519 TFA inhibits tumor growth in a human MM xenograft mouse model[1]. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) TFA also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice[2].

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

分子量

496.27

Formula

C18H18Cl2F3N5O4
CAS 号

1431697-85-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献

  • [1]. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36.

    [2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines.

    [3]. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8.
Cell Assay
[1]

AT7519’s effects on viability of MM cell lines, primary MM cells, and PBMNCs is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrasodium bromide (MTT) dye absorbance. DNA synthesis is measured by tritiated thymidine uptake (3H-TdR). MM cells (2-3 × 104 cells/well) are incubated in 96-well culture plates with media and different concentrations of AT7519 and/or recombinant IL-6 (10 ng/mL) or IGF-1 (50 ng/mL) for 24 or 48 h at 37°C and 3H-TdR incorporation is measured.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

To evaluate the in vivo anti-MM activity of AT7519, male SCID mice are inoculated subcutaneously with 5×106 MM.1S cells in 100 μL serum-free RPMI 1640 medium. When tumors are measurable, mice are treated intraperitoneally (IP) with vehicle or AT7519 dissolved in saline 0.9%. The first group of 10 mice is treated with 15 mg/kg once a day for five days for 2 weeks, and the second group is treated with 15 mg/kg once a day three times a week for four consecutive weeks. The control group receives the carrier alone at the same schedule. Tumor size is measured every alternate day in 2 dimensions using calipers, and tumor volume is calculated with the formula: V= 0.5 a × b2 (a= long diameter of the tumor, b= short diameter of the tumor). Animals are sacrificed when the tumor reaches 2 cm3 or when the tumor is ulcerated. Survival and tumor growth are evaluated from the first day of treatment until death.

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

  • [1]. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36.

    [2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines.

    [3]. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

AT7519(Synonyms: AT7519M)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

AT7519 (Synonyms: AT7519M) 纯度: 99.76%

AT7519 (AT7519M) 是一种有效的 CDK 抑制剂，对 CDK1，CDK2，CDK4-CDK6 以及 CDK9 的 IC50 值分别为 210，47，100，13，170 和 <10 nM。

AT7519(Synonyms: AT7519M)

AT7519 Chemical Structure

CAS No. : 844442-38-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥891 In-stock
5 mg ￥810 In-stock
10 mg ￥1350 In-stock
50 mg ￥4450 In-stock
100 mg ￥6900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AT7519 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

AT7519 (AT7519M) as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

IC50 & Target[2]

CDK9/Cyclin T

10 nM (IC50)

CDK5/p35

13 nM (IC50)

cdk2/cyclin A

47 nM (IC50)

Cdk4/cyclin D1

100 nM (IC50)

cdk6/cyclin D3

170 nM (IC50)

Cdk1/cyclin B

210 nM (IC50)

CDK7/Cyclin H/MAT1

2400 nM (IC50)

GSK3β

89 nM (IC50)

体外研究
(In Vitro)

AT7519 (0-4 μM) results in dose-dependent cytotoxicity with IC50s ranging from 0.5 to 2 μM in MM cells, and this induced cytotoxicity is associated with GSK-3β activation independent of transcriptional inhibition. AT7519 overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells[1]. AT7519 (250 nM) inhibits cell cycle progression in human tumor cell lines. AT7519 also induces apoptosis of human tumor cell lines[2]. AT7519 (100-700 nM) induces apoptosis in leukemia cell lines. AT7519 also inhibits transcription in human tumor cell lines. Furthermore, AT7519 inhibits RNA polymerase II and reduces antiapoptotic protein levels[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

AT7519 inhibits tumor growth in a human MM xenograft mouse model[1]. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

382.24

Formula

C16H17Cl2N5O2
CAS 号

844442-38-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (130.81 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6162 mL 13.0808 mL 26.1616 mL
5 mM 0.5232 mL 2.6162 mL 5.2323 mL
10 mM 0.2616 mL 1.3081 mL 2.6162 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.54 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.54 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.54 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36.

    [2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines.

    [3]. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8.
Cell Assay
[1]

AT7519’s effects on viability of MM cell lines, primary MM cells, and PBMNCs is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrasodium bromide (MTT) dye absorbance. DNA synthesis is measured by tritiated thymidine uptake (3H-TdR). MM cells (2-3 × 104 cells/well) are incubated in 96-well culture plates with media and different concentrations of AT7519 and/or recombinant IL-6 (10 ng/mL) or IGF-1 (50 ng/mL) for 24 or 48 h at 37°C and 3H-TdR incorporation is measured.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

To evaluate the in vivo anti-MM activity of AT7519, male SCID mice are inoculated subcutaneously with 5×106 MM.1S cells in 100 μL serum-free RPMI 1640 medium. When tumors are measurable, mice are treated intraperitoneally (IP) with vehicle or AT7519 dissolved in saline 0.9%. The first group of 10 mice is treated with 15 mg/kg once a day for five days for 2 weeks, and the second group is treated with 15 mg/kg once a day three times a week for four consecutive weeks. The control group receives the carrier alone at the same schedule. Tumor size is measured every alternate day in 2 dimensions using calipers, and tumor volume is calculated with the formula: V= 0.5 a × b2 (a= long diameter of the tumor, b= short diameter of the tumor). Animals are sacrificed when the tumor reaches 2 cm3 or when the tumor is ulcerated. Survival and tumor growth are evaluated from the first day of treatment until death.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36.

    [2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines.

    [3]. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

ATM-3507 trihydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ATM-3507 trihydrochloride  纯度: 98.10%

ATM-3507 trihydrochloride 是原肌球蛋白 (tropomyosin) 的一个有效抑制剂，其在人类黑色素瘤细胞系中的 IC50 值约为 3.83-6.84 μM。

ATM-3507 trihydrochloride

ATM-3507 trihydrochloride Chemical Structure

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2142 In-stock
5 mg ￥1350 In-stock
10 mg ￥2300 In-stock
50 mg ￥7000 In-stock
100 mg ￥12000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

ATM-3507 trihydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Cytoskeleton Compound Library
  • Targeted Diversity Library

生物活性

ATM-3507 trihydrochloride is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.

IC50 & Target

IC50: 3.83-6.84 μM (tropomyosin, in human melanoma celllines)[1].
体内研究
(In Vivo)

The maximal tolerance dose (MTD) for TR100 and ATM-3507 is 60 and 150 mg/kg, respectively. It is found that a significant inhibition of tumor growth and prolongation of animal survival using either combination compared with each monotherapy. The median survival of mice increased from 18 days for mice treated with ATM-3507 to more than 49 days for mice treated with the combination. It is also found that twice weekly intravenous administration of ATM-3507 also show combination efficacy. The impact of each treatment or the combination on body weight is minimal. Drug levels are measured following the intravenous administration of ATM-3507 at 30 mg/kg in Balb/c mice (n=3 per time point). The mean half-life of ATM-3507 is 5.01 hrs for the terminal elimination phase. The mean AUC0-t in the plasma is 14,548 ng/h/mL. The Cmax of ATM-3507 is 5,758 ng/mL and the the t1/2 is 5.01 h. The observed plasma clearance and volume of distribution at steady state of ATM-3507 is 33.8 mL/min/kg and 7.23 L/kg, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

721.17

Formula

C37H49Cl3FN5O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (346.66 mM; Need ultrasonic)

H2O : 33.33 mg/mL (46.22 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3866 mL 6.9332 mL 13.8664 mL
5 mM 0.2773 mL 1.3866 mL 2.7733 mL
10 mM 0.1387 mL 0.6933 mL 1.3866 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.88 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.88 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (2.88 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.88 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Currier MA, et al. Identification of Cancer-Targeted Tropomyosin Inhibitors and Their Synergy with Microtubule Drugs.Mol Cancer Ther. 2017 Aug;16(8):1555-1565.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务