标签归档：dasatinib

Dasatinib hydrochloride(Synonyms: 达沙替尼盐酸盐; BMS-354825 hydrochloride)

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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。

Dasatinib hydrochloride (Synonyms: 达沙替尼盐酸盐; BMS-354825 hydrochloride) 纯度: 98.64%

Dasatinib (BMS-354825) hydrochloride 是一种具有口服活性的，ATP 竞争性的，双重 Src/Bcr-Abl 抑制剂，具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的 Ki 值分别为 16 pM 和 30 pM。Dasatinib hydrochloride 抑制 Bcr-Abl 和 Src 的IC50 分别为 <1.0 nM 和 0.5 nM。Dasatinib hydrochloride 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。

Dasatinib hydrochloride(Synonyms: 达沙替尼盐酸盐; BMS-354825 hydrochloride)

Dasatinib hydrochloride Chemical Structure

CAS No. : 854001-07-3

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  • Neurodegenerative Disease-related Compound Library
  • Angiogenesis Related Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively[1]. Dasatinib hydrochloride also induces apoptosis and autophagy.

IC50 & Target[1]

Bcr-Abl

1.0 nM (IC50)

Src

0.5 nM (IC50)

lck

0.4 nM (IC50)

Yes

0.5 nM (IC50)

c-kit

5.0 nM (IC50)

PDGFRβ

28 nM (IC50)

p38

100 nM (IC50)

Her1

180 nM (IC50)

Her2

710 nM (IC50)

FGFR-1

880 nM (IC50)

MEK

1700 nM (IC50)

体外研究
(In Vitro)

Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively[1].
Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, 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)

Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels[1].
Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%[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: Nude mice bearing K562 xenografts
Dosage: 5 mg/kg and 50 mg/kg
Administration: Oral administration on a 5 day on and 2 day off schedule.
Result: Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
Animal Model: Sprague-Dawley Rats
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: Oral and i.v.
Result: Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively.

Clinical Trial

分子量

524.47

Formula

C22H27Cl2N7O2S
CAS 号

854001-07-3
中文名称

达沙替尼盐酸盐；盐酸达沙替尼
运输条件

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

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 15 mg/mL (28.60 mM; Need ultrasonic and warming)

H2O : 10 mg/mL (19.07 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9067 mL 9.5334 mL 19.0669 mL
5 mM 0.3813 mL 1.9067 mL 3.8134 mL
10 mM 0.1907 mL 0.9533 mL 1.9067 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 (stored under nitrogen)。-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: ≥ 3.33 mg/mL (6.35 mM); Clear solution

    此方案可获得 ≥ 3.33 mg/mL (6.35 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 33.3 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: ≥ 3.33 mg/mL (6.35 mM); Clear solution

    此方案可获得 ≥ 3.33 mg/mL (6.35 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 33.3 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: ≥ 3.33 mg/mL (6.35 mM); Clear solution

    此方案可获得 ≥ 3.33 mg/mL (6.35 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 33.3 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]. Lombardo LJ, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61.

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N-Deshydroxyethyl Dasatinib-d8

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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。

N-Deshydroxyethyl Dasatinib-d8 

N-Deshydroxyethyl Dasatinib-d8 是 N-Deshydroxyethyl Dasatinib 的氘代物。N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) 是一种基于 Dasatinib (ABL 抑制剂) 的配体，可通过 linker 与 IAP 配体结合从而形成 SNIPER 分子，从而降解 ABL。

N-Deshydroxyethyl Dasatinib-d8

N-Deshydroxyethyl Dasatinib-d8 Chemical Structure

CAS No. : 1189998-96-6

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生物活性

N-Deshydroxyethyl Dasatinib-d8 is the deuterium labeled N-Deshydroxyethyl Dasatinib. N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825), the Dasatinib-based moiety, binds to IAP ligand via a linker to form SNIPER to degrade ABL[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

452.00

Formula

C20H14D8ClN7OS
CAS 号

1189998-96-6
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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Dasatinib N-oxide-d8(Synonyms: 达沙替尼 N 氧化物 d8)

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。

Dasatinib N-oxide-d8 (Synonyms: 达沙替尼 N 氧化物 d8)

Dasatinib N-oxide-d8 是 Dasatinib N-oxide 的氘代物。Dasatinib N-oxide 是 Dasatinib 的次要代谢物。Dasatinib 是一种有效且具有口服活性的双重 Src/Bcr-Abl 抑制剂。

Dasatinib N-oxide-d8(Synonyms: 达沙替尼 N 氧化物 d8)

Dasatinib N-oxide-d8 Chemical Structure

CAS No. : 1189988-36-0

规格 是否有货
1 mg Check price and availability
5 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Dasatinib N-oxide-d8 is the deuterium labeled Dasatinib N-oxide. Dasatinib N-oxide is a minor metabolite of Dasatinib. Dasatinib is a potent and orally active dual Src/Bcr-Abl inhibitor[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

512.05

Formula

C22H18D8ClN7O3S
CAS 号

1189988-36-0
中文名称

达沙替尼 N 氧化物 d8
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Christopher LJ, et, al. Metabolism and disposition of dasatinib after oral administration to humans. Drug Metab Dispos. 2008 Jul;36(7):1357-64.

    [3]. Furlong MT, et, al. A validated LC-MS/MS assay for the simultaneous determination of the anti-leukemic agent dasatinib and two pharmacologically active metabolites in human plasma: application to a clinical pharmacokinetic study. J Pharm Biomed Anal. 2012 Jan 25;58:130-5.

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Dasatinib carbaldehyde(Synonyms: BMS-354825 carbaldehyde; PROTAC ABL binding moiety 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。

Dasatinib carbaldehyde (Synonyms: BMS-354825 carbaldehyde; PROTAC ABL binding moiety 4)

Dasatinib carbaldehyde (BMS-354825 carbaldehyde) 是一种基于 Dasatinib (ABL 抑制剂) 的配体，可通过 linker 与 IAP 配体结合从而形成 SNIPER 分子。

Dasatinib carbaldehyde(Synonyms: BMS-354825 carbaldehyde; PROTAC ABL binding moiety 4)

Dasatinib carbaldehyde Chemical Structure

CAS No. : 2112837-79-1

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER [1].

分子量

471.96

Formula

C21H22ClN7O2S
CAS 号

2112837-79-1
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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

Dasatinib(Synonyms: 达沙替尼; BMS-354825)

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。

Dasatinib (Synonyms: 达沙替尼; BMS-354825) 纯度: 99.83%

Dasatinib (BMS-354825) 是一种具有口服活性的，ATP 竞争性的，双重 Src/Bcr-Abl 抑制剂，具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的 Ki 值分别为 16 pM 和 30 pM。Dasatinib 抑制 Bcr-Abl 和 Src 的IC50 分别为 <1.0 nM 和 0.5 nM。Dasatinib 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。

Dasatinib(Synonyms: 达沙替尼; BMS-354825)

Dasatinib Chemical Structure

CAS No. : 302962-49-8

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 ￥968 In-stock
50 mg ￥880 In-stock
100 mg ￥1200 In-stock
200 mg ￥1650 In-stock
500 mg ￥2400 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Dasatinib 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Autophagy Compound Library
  • Drug Repurposing Compound Library
  • Reprogramming Compound Library
  • Anti-COVID-19 Compound Library
  • NMPA-Approved Drug Library
  • Cytoskeleton Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Alzheimer’s Disease Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Therapy Drug Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Angiogenesis Related Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively[1]. Dasatinib also induces apoptosis and autophagy.

IC50 & Target[1]

Bcr-Abl

1.0 nM (IC50)

Src

0.5 nM (IC50)

lck

0.4 nM (IC50)

yes

0.5 nM (IC50)

c-kit

5.0 nM (IC50)

PDGFRβ

28 nM (IC50)

p38

100 nM (IC50)

Her1

180 nM (IC50)

Her2

710 nM (IC50)

FGFR-1

880 nM (IC50)

MEK

1700 nM (IC50)

体外研究
(In Vitro)

Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively[1].
Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, 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)

Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels[1].
Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%[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: Nude mice bearing K562 xenografts
Dosage: 5 mg/kg and 50 mg/kg
Administration: Oral administration on a 5 day on and 2 day off schedule.
Result: Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
Animal Model: Sprague-Dawley Rats
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: Oral and i.v.
Result: Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively.

Clinical Trial

分子量

488.01

Formula

C22H26ClN7O2S
CAS 号

302962-49-8
中文名称

达沙替尼
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 : 250 mg/mL (512.28 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0491 mL 10.2457 mL 20.4914 mL
5 mM 0.4098 mL 2.0491 mL 4.0983 mL
10 mM 0.2049 mL 1.0246 mL 2.0491 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： 0.5% MC  0.5% Tween-80

    Solubility: 6.67 mg/mL (13.67 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

  • 3.

    请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

  • 4.

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

    Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.26 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

  • 5.

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

    Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.26 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
  • 6.

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

    Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.26 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 20.8 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]. Lombardo LJ, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61.

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Dasatinib-d8(Synonyms: BMS-354825-d8)

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。

Dasatinib-d8 (Synonyms: BMS-354825-d8)

Dasatinib D8 是氘标记的Dasatinib。Dasatinib 是 Bcr-Abl 和 Src 家族酪氨酸激酶双抑制剂。

Dasatinib-d8(Synonyms: BMS-354825-d8)

Dasatinib-d8 Chemical Structure

CAS No. : 1132093-70-9

规格 价格 是否有货
1 mg ￥3100 询问价格 & 货期
5 mg ￥9500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Dasatinib D8 is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

分子量

496.05

Formula

C22H18D8ClN7O2S
CAS 号

1132093-70-9
中文名称

达沙替尼 d8
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.

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

Dasatinib N-oxide(Synonyms: 达沙替尼N氧化物；达沙替尼杂质)

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。

Dasatinib N-oxide (Synonyms: 达沙替尼N氧化物；达沙替尼杂质) 纯度: 99.27%

Dasatinib N-oxide 是 Dasatinib 的次要代谢物。Dasatinib 是一种有效且具有口服活性的双重 Src/Bcr-Abl 抑制剂。

Dasatinib N-oxide(Synonyms: 达沙替尼N氧化物；达沙替尼杂质)

Dasatinib N-oxide Chemical Structure

CAS No. : 910297-52-8

规格 价格 是否有货 数量
5 mg ￥2500 In-stock
10 mg ￥4200 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Dasatinib N-oxide 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Drug Metabolite Library

生物活性

Dasatinib N-oxide is a minor metabolite of Dasatinib. Dasatinib is a potent and orally active dual Src/Bcr-Abl inhibitor[1][2].

体内研究
(In Vivo)

Dasatinib N-oxide is the pharmacologically active metabolite after oral administration[1].

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

504.00

Formula

C22H26ClN7O3S
CAS 号

910297-52-8
中文名称

达沙替尼N氧化物；达沙替尼杂质
运输条件

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

4°C, protect from light

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

DMSO : 8.33 mg/mL (16.53 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9841 mL 9.9206 mL 19.8413 mL
5 mM 0.3968 mL 1.9841 mL 3.9683 mL
10 mM 0.1984 mL 0.9921 mL 1.9841 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 (protect from 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。

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 (1.65 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.65 mM，饱和度未知) 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 (1.65 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.65 mM，饱和度未知) 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 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 (1.65 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.65 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 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Christopher LJ, et, al. Metabolism and disposition of dasatinib after oral administration to humans. Drug Metab Dispos. 2008 Jul;36(7):1357-64.

    [2]. Furlong MT, et, al. A validated LC-MS/MS assay for the simultaneous determination of the anti-leukemic agent dasatinib and two pharmacologically active metabolites in human plasma: application to a clinical pharmacokinetic study. J Pharm Biomed Anal. 2012 Jan 25;58:130-5.

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

Dasatinib monohydrate(Synonyms: BMS-354825 monohydrate)

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。

Dasatinib monohydrate (Synonyms: BMS-354825 monohydrate)

Dasatinib (BMS-354825) monohydrate 是一种具有口服活性的，ATP 竞争性的，双重 Src/Bcr-Abl 抑制剂，具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的 Ki 值分别为 16 pM 和 30 pM。Dasatinib monohydrate 抑制 Bcr-Abl 和 Src 的IC50 分别为 <1.0 nM 和 0.5 nM。Dasatinib monohydrate 还诱导凋亡 (apoptosis) 和自噬 (autophagy)。

Dasatinib monohydrate(Synonyms: BMS-354825 monohydrate)

Dasatinib monohydrate Chemical Structure

CAS No. : 863127-77-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Dasatinib monohydrate 的其他形式现货产品:

Dasatinib Dasatinib hydrochloride

生物活性

Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively[1]. Dasatinib monohydrate also induces apoptosis and autophagy.

IC50 & Target[1]

Bcr-Abl

1.0 nM (IC50)

Src

0.5 nM (IC50)

lck

0.4 nM (IC50)

yes

0.5 nM (IC50)

c-kit

5.0 nM (IC50)

PDGFRβ

28 nM (IC50)

p38

100 nM (IC50)

Her1

180 nM (IC50)

Her2

710 nM (IC50)

FGFR-1

880 nM (IC50)

MEK

1700 nM (IC50)

体外研究
(In Vitro)

Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively[1].
Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively[1].

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)

Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels[1].
Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%[1].

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

Animal Model: Nude mice bearing K562 xenografts
Dosage: 5 mg/kg and 50 mg/kg
Administration: Oral administration on a 5 day on and 2 day off schedule.
Result: Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
Animal Model: Sprague-Dawley Rats
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: Oral and i.v.
Result: Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively.

Clinical Trial

分子量

506.02

Formula

C22H28ClN7O3S
CAS 号

863127-77-9
中文名称

达沙替尼一水合物
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]. Lombardo LJ, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61.

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