标签归档：tosylate

Niraparib tosylate hydrate(Synonyms: MK-4827 tosylate hydrate)

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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。

Niraparib tosylate hydrate (Synonyms: MK-4827 tosylate hydrate)

Niraparib (MK-4827) tosylate hydrate 是高效的，具有生物口服利用度的 PARP1 和 PARP2 抑制剂，IC50 分别为 3.8 nM 和 2.1 nM。Niraparib tosylate hydrate 抑制 DNA 损伤修复，诱导凋亡 (apoptosis) 并具有抗肿瘤活性。

Niraparib tosylate hydrate(Synonyms: MK-4827 tosylate hydrate)

Niraparib tosylate hydrate Chemical Structure

CAS No. : 1613220-15-7

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Niraparib tosylate hydrate 的其他形式现货产品:

Niraparib Niraparib tosylate

生物活性

Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].

IC50 & Target

PARP-2

2.1 nM (IC50)

PARP-1

3.8 nM (IC50)

V-PARP

330 nM (IC50)

TANK-1

570 nM (IC50)

PARP-3

1300 nM (IC50)

体外研究
(In Vitro)

Niraparib (MK-4827) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay[1].
To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells[2].

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)

Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%[1].
Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily[3].

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

510.61

Formula

C26H30N4O5S
CAS 号

1613220-15-7
中文名称

甲苯磺酸尼拉帕尼一水物
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]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

    [2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.

    [3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.

    [4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.
Cell Assay

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

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

  • [1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

    [2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.

    [3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.

    [4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.

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AZD3229 Tosylate

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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。

AZD3229 Tosylate  纯度: 98.54%

AZD3229 Tosylate 是一种有效的、广泛的突变型酪氨酸激酶受体 (KIT) 抑制剂，可用于开发研究胃肠道间质瘤。

AZD3229 Tosylate

AZD3229 Tosylate Chemical Structure

CAS No. : 2248003-71-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥1850 In-stock
10 mg ￥2900 In-stock
25 mg ￥5300 In-stock
50 mg ￥8800 In-stock
100 mg ￥14800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AZD3229 Tosylate 相关产品

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  • Bioactive Compound Library Plus
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生物活性

AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.

IC50 & Target

KIT[1].
体外研究
(In Vitro)

AZD3229 is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM). AZD3229 demonstrates potent single digit nM growth inhibition across a broad cell panel, with good margin to KDR-driven effects. Selectivity over KDR can be rationalised predominantly by the interaction of water molecules with the protein and ligand in the active site and its kinome selectivity is similar to the best of the approved GIST agents[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

651.71

Formula

C31H34FN7O6S
CAS 号

2248003-71-4
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 : ≥ 100 mg/mL (153.44 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 1.5344 mL 7.6721 mL 15.3442 mL
5 mM 0.3069 mL 1.5344 mL 3.0688 mL
10 mM 0.1534 mL 0.7672 mL 1.5344 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。
参考文献

  • [1]. Kettle JG, et al. Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. J Med Chem. 2018 Oct 11;61(19):8797-8810.

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Edoxaban tosylate(Synonyms: 依度沙班对甲苯磺酸盐; DU-176b)

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。

Edoxaban tosylate (Synonyms: 依度沙班对甲苯磺酸盐; DU-176b) 纯度: 99.47%

Edoxaban tosylate (DU-176b) 是一种选择性，有效和口服活性的 factor Xa (FXa) 抑制剂，对游离 FXa 和凝血酶原的 Ki 分别为 0.561 nM 和 2.98 nM。Edoxaban tosylate 是一种抗凝剂，可用于预防中风。Edoxaban tosylate 还是一种凝血酶和凝血因子 IXaβ (FIXa) 的弱抑制剂，Ki 值分别为 6.00 μM 和 41.7 μM，对 FXa 的选择性超过 10000 倍。Edoxaban tosylate 具有抗血栓形成的特性，可用于血栓栓塞性疾病的研究。

Edoxaban tosylate(Synonyms: 依度沙班对甲苯磺酸盐; DU-176b)

Edoxaban tosylate Chemical Structure

CAS No. : 480449-71-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1743 In-stock
5 mg ￥1100 In-stock
10 mg ￥1900 In-stock
50 mg ￥6900 In-stock
100 mg ￥9950 In-stock
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500 mg   询价  

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  • Drug Repurposing Compound Library
  • Anti-Cardiovascular Disease Compound Library
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  • Orally Active Compound Library
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  • FDA-Approved Anticancer Drug Library

生物活性

Edoxaban tosylate (DU-176b) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate has antithrombotic properties and has potential for thromboembolic diseases treatment[1][2][3].

IC50 & Target

Ki: 0.561 nM (Free FXa); 2.98 nM (Prothrombinase); 6.00 μM (Thrombin) and 41.7 μM (Factor IXaβ)[1]
体外研究
(In Vitro)

Edoxaban (DU-176b) also inhibits rat, cynomolgus monkey and rabbit FXa with Ki values of 6.90 nM, 0.715 nM and 0.457 nM, respectively[1].
Prothrombin time (PT), activated partial thromboplastin time (APTT) and thrombin time (TT) of human plasma are prolonged by Edoxaban (DU-176b) in a concentration-dependent manner, doubling PT and APTT at 0.256 and 0.508 μM, respectively. The double clotting time (CT2) for TT, however, was much higher (4.95 μM), reflecting its anti-thrombin activity. Thrombin-induced platelet aggregation is inhibited by a high concentration of Edoxaban (DU-176b) (IC50: 2.90 μM), reflecting its weak anti-thrombin activity[1].
Edoxaban is minimally metabolized (,4%) by the cytochrome P450 system (CYP3A4) and is a substrate for P-glycoprotein[2].

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)

Edoxaban (DU-176b; 0.5-12.5 mg/kg; oral administration; Wistar rats) dose-dependently inhibits thrombus formation in rat thrombosis models[1].

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

Animal Model: Wistar rats (210-240 g) with venous stasis thrombosis model[1]
Dosage: 0.5 mg/kg, 2.5 mg/kg, 12.5 mg/kg
Administration: Oral administration
Result: Dose-dependently inhibited thrombus formation in rat thrombosis models.

Clinical Trial

分子量

720.26

Formula

C31H38ClN7O7S2
CAS 号

480449-71-6
中文名称

依度沙班对甲苯磺酸盐；伊多塞班对甲苯磺酸盐
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 : 100 mg/mL (138.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3884 mL 6.9419 mL 13.8839 mL
5 mM 0.2777 mL 1.3884 mL 2.7768 mL
10 mM 0.1388 mL 0.6942 mL 1.3884 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: ≥ 2.5 mg/mL (3.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.47 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 (3.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.47 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 (3.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.47 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9.

    [2]. Mendell J, Lee F, Chen S, The Effects of the Antiplatelet Agents, Aspirin and Naproxen, on Pharmacokinetics and Pharmacodynamics of the Anticoagulant Edoxaban, a Direct Factor Xa Inhibitor. J Cardiovasc Pharmacol. 2013 Apr 23. [Epub ahead of print]

    [3]. Stacy ZA, et al. Edoxaban: A Comprehensive Review of the Pharmacology and Clinical Data for the Management of Atrial Fibrillation and Venous Thromboembolism. Cardiol Ther. 2016 Jun;5(1):1-18.

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