标签归档：alectinib

生物活性分子抑制剂Alectinib Hydrochloride(Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)

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。

Alectinib Hydrochloride (Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 纯度: 99.89%

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 是一种有效，选择性和口服的 ALK 抑制剂，其 IC50 为 1.9 nM，Kd 值为 2.4 nM (以 ATP 竞争方式)，并且还抑制 ALK F1174L 和 ALK R1275Q，其 IC50 分别为 1 nM 和 3.5 nM。Alectinib Hydrochloride 还具有有效的中枢神经系统 (CNS) 渗透能力。

Alectinib Hydrochloride(Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)

Alectinib Hydrochloride Chemical Structure

CAS No. : 1256589-74-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
2 mg ￥520 In-stock
5 mg ￥1000 In-stock
10 mg ￥1500 In-stock
50 mg ￥4500 In-stock
100 mg ￥7000 In-stock
200 mg ￥13000 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Alectinib Hydrochloride 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
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Drug Repurposing Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Lung Cancer Compound Library
  • Targeted Therapy Drug Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

IC50 & Target

IC50: 1.9 nM (ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]
Kd: 2.4 nM (ALK)[1]
体外研究
(In Vitro)

Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT[1].
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner[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.

Western Blot Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 0 nM,10 nM,100 nM, 1000 nM
Incubation Time: 2 hours
Result: Inhibition of ALK phosphorylation and signal transduction.

Cell Viability Assay[1]

Cell Line: HCC827, A549, or NCIH522 cells
Concentration: 0-1000 nM
Incubation Time: 5 days
Result: Reduced cell activity in a dose-dependent manner.

体内研究
(In Vivo)

Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed[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: SCID or nude mice bearing NCI-H2228 cells[1]
Dosage: 0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
Administration: Oral administration; once daily; for 11 days
Result: Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.

Clinical Trial

分子量

519.08

Formula

C30H35ClN4O2
CAS 号

1256589-74-8
中文名称

艾乐替尼盐酸盐；盐酸阿雷替尼
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 : 5 mg/mL (9.63 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9265 mL 9.6324 mL 19.2649 mL
5 mM 0.3853 mL 1.9265 mL 3.8530 mL
10 mM — — —

*

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]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690.

    [2]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222.

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

生物活性分子抑制剂Alectinib Hydrochloride(Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)

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。
Alectinib Hydrochloride (Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 纯度: 99.89%

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) 是一种有效，选择性和口服的 ALK 抑制剂，其 IC50 为 1.9 nM，Kd 值为 2.4 nM (以 ATP 竞争方式)，并且还抑制 ALK F1174L 和 ALK R1275Q，其 IC50 分别为 1 nM 和 3.5 nM。Alectinib Hydrochloride 还具有有效的中枢神经系统 (CNS) 渗透能力。

Alectinib Hydrochloride(Synonyms: 艾乐替尼盐酸盐; CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride)

Alectinib Hydrochloride Chemical Structure

CAS No. : 1256589-74-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
2 mg ￥520 In-stock
5 mg ￥1000 In-stock
10 mg ￥1500 In-stock
50 mg ￥4500 In-stock
100 mg ￥7000 In-stock
200 mg ￥13000 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Alectinib Hydrochloride 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
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • CNS-Penetrant Compound Library
  • Drug Repurposing Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Lung Cancer Compound Library
  • Targeted Therapy Drug Library
  • Rare Diseases Drug Library
  • Children’s Drug Library

生物活性

Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

IC50 & Target

IC50: 1.9 nM (ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]
Kd: 2.4 nM (ALK)[1]
体外研究
(In Vitro)

Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT[1].
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner[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.

Western Blot Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 0 nM,10 nM,100 nM, 1000 nM
Incubation Time: 2 hours
Result: Inhibition of ALK phosphorylation and signal transduction.

Cell Viability Assay[1]

Cell Line: HCC827, A549, or NCIH522 cells
Concentration: 0-1000 nM
Incubation Time: 5 days
Result: Reduced cell activity in a dose-dependent manner.

体内研究
(In Vivo)

Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed[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: SCID or nude mice bearing NCI-H2228 cells[1]
Dosage: 0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
Administration: Oral administration; once daily; for 11 days
Result: Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.

Clinical Trial

分子量

519.08

Formula

C30H35ClN4O2
CAS 号

1256589-74-8
中文名称

艾乐替尼盐酸盐；盐酸阿雷替尼
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 : 5 mg/mL (9.63 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9265 mL 9.6324 mL 19.2649 mL
5 mM 0.3853 mL 1.9265 mL 3.8530 mL
10 mM — — —

*

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]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690.

    [2]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222.

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

Alectinib-d8(Synonyms: CH5424802-d8; RO5424802-d8; AF802-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。

Alectinib-d8 (Synonyms: CH5424802-d8; RO5424802-d8; AF802-d8)

Alectinib-d8 (CH5424802-d8) 是 Alectinib 的氘代物。Alectinib (CH5424802) 是一种有效、选择性、具有口服活性的 ALK 抑制剂，其 IC50 为 1.9 nM，Kd 值为 2.4 nM (以 ATP 竞争方式)，并且还抑制 ALK F1174L 和 ALK R1275Q，其 IC50 分别为 1 nM

Alectinib-d8(Synonyms: CH5424802-d8; RO5424802-d8; AF802-d8)

Alectinib-d8 Chemical Structure

CAS No. : 1256585-15-5

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

* Please select Quantity before adding items.

生物活性

Alectinib-d8 (CH5424802-d8) is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[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

490.67

Formula

C30H26D8N4O2
CAS 号

1256585-15-5
中文名称

艾乐替尼 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.
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]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690.

    [3]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222.

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

Alectinib-d8(Synonyms: CH5424802-d8; RO5424802-d8; AF802-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。

Alectinib-d8 (Synonyms: CH5424802-d8; RO5424802-d8; AF802-d8)

Alectinib-d8 (CH5424802-d8) 是 Alectinib 的氘代物。Alectinib (CH5424802) 是一种有效、选择性、具有口服活性的 ALK 抑制剂，其 IC50 为 1.9 nM，Kd 值为 2.4 nM (以 ATP 竞争方式)，并且还抑制 ALK F1174L 和 ALK R1275Q，其 IC50 分别为 1 nM

Alectinib-d8(Synonyms: CH5424802-d8; RO5424802-d8; AF802-d8)

Alectinib-d8 Chemical Structure

CAS No. : 1256585-15-5

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

* Please select Quantity before adding items.

生物活性

Alectinib-d8 (CH5424802-d8) is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[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

490.67

Formula

C30H26D8N4O2
CAS 号

1256585-15-5
中文名称

艾乐替尼 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.
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]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690.

    [3]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222.

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

Alectinib-d8(Synonyms: CH5424802-d8; RO5424802-d8; AF802-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。

Alectinib-d8 (Synonyms: CH5424802-d8; RO5424802-d8; AF802-d8)

Alectinib-d8 (CH5424802-d8) 是 Alectinib 的氘代物。Alectinib (CH5424802) 是一种有效、选择性、具有口服活性的 ALK 抑制剂，其 IC50 为 1.9 nM，Kd 值为 2.4 nM (以 ATP 竞争方式)，并且还抑制 ALK F1174L 和 ALK R1275Q，其 IC50 分别为 1 nM

Alectinib-d8(Synonyms: CH5424802-d8; RO5424802-d8; AF802-d8)

Alectinib-d8 Chemical Structure

CAS No. : 1256585-15-5

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

* Please select Quantity before adding items.

生物活性

Alectinib-d8 (CH5424802-d8) is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[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].

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

490.67

Formula

C30H26D8N4O2
CAS 号

1256585-15-5
中文名称

艾乐替尼 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.
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]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690.

    [3]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222.

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

Alectinib-d6(Synonyms: CH5424802-d6; RO5424802-d6; AF802-d6)

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。

Alectinib-d6 (Synonyms: CH5424802-d6; RO5424802-d6; AF802-d6)

Alectinib-d6 是 Alectinib 氘代物。Alectinib (CH5424802) 是一种有效、选择性、具有口服活性的 ALK 抑制剂，其 IC50 为 1.9 nM，Kd 值为 2.4 nM (以 ATP 竞争方式)，并且还抑制 ALK F1174L 和 ALK R1275Q，其 IC50 分别为 1 nM 和 3.5 nM。Alectinib 还具有有效的中枢神经系统 (CNS) 渗透能力。

Alectinib-d6(Synonyms: CH5424802-d6; RO5424802-d6; AF802-d6)

Alectinib-d6 Chemical Structure

CAS No. : 1616374-19-6

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

* Please select Quantity before adding items.

生物活性

Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[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

488.65

Formula

C30H28D6N4O2
CAS 号

1616374-19-6
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]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690.

    [3]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222.

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

Alectinib(Synonyms: 艾乐替尼; CH5424802; RO5424802; AF802)

发表于由

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Alectinib (Synonyms: 艾乐替尼; CH5424802; RO5424802; AF802) 纯度: 99.87%

Alectinib (CH5424802) 是一种有效、选择性、具有口服活性的 ALK 抑制剂，其 IC50 为 1.9 nM，Kd 值为 2.4 nM (以 ATP 竞争方式)，并且还抑制 ALK F1174L 和 ALK R1275Q，其 IC50 分别为 1 nM 和 3.5 nM。Alectinib 还具有有效的中枢神经系统 (CNS) 渗透能力。

Alectinib(Synonyms: 艾乐替尼; CH5424802; RO5424802; AF802)

Alectinib Chemical Structure

CAS No. : 1256580-46-7

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10 mM * 1 mL in DMSO ￥902 In-stock
2 mg ￥520 In-stock
5 mg ￥850 In-stock
10 mg ￥1400 In-stock
50 mg ￥4000 In-stock
100 mg ￥6500 In-stock
200 mg ￥12000 In-stock
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生物活性

Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].

IC50 & Target

IC50: 1.9 nM(ALK), 1 nM (ALKF1174L), 3.5 nM (ALKR1275Q)[1]
Kd: 2.4 nM (ALK)[1]
体外研究
(In Vitro)

Alectinib (0-1000 nM; 2 hours; NCI-H2228 cells) treatment could prevent autophosphorylation of ALK in NCI-H2228 cells expressing EML4-ALK, and it also resulted in substantial suppression of phosphorylation of STAT3 and AKT[1].
Alectinib (0-1000 nM; 5 days; HCC827, A549, or NCIH522 cells) treatment reduces cell activity in a dose-dependent manner[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.

Western Blot Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 0 nM,10 nM,100 nM, 1000 nM
Incubation Time: 2 hours
Result: Inhibition of ALK phosphorylation and signal transduction.

Cell Viability Assay[1]

Cell Line: HCC827, A549, or NCIH522 cells
Concentration: 0-1000 nM
Incubation Time: 5 days
Result: Reduced cell activity in a dose-dependent manner.

体内研究
(In Vivo)

Alectinib (0.2-20 mg/kg; oral administration; once daily; for 11 days; SCID or nude mice bearing NCI-H2228 cells) treatment can result in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression. At any dose level, no differences in body weight or gross signs of toxicity are observed[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: SCID or nude mice bearing NCI-H2228 cells[1]
Dosage: 0.2 mg/kg, 0.6 mg/kg, 2 mg/kg, 6 mg/kg, 20 mg/kg
Administration: Oral administration; once daily; for 11 days
Result: Resulted in dose-dependent tumor growth inhibition (EC50 of 0.46 mg/kg) and tumor regression.

Clinical Trial

分子量

482.62

Formula

C30H34N4O2
CAS 号

1256580-46-7
中文名称

艾乐替尼；阿雷替尼
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 : 6.2 mg/mL (12.85 mM; Need warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0720 mL 10.3601 mL 20.7202 mL
5 mM 0.4144 mL 2.0720 mL 4.1440 mL
10 mM 0.2072 mL 1.0360 mL 2.0720 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% CMC-Na/saline water

    Solubility: 20 mg/mL (41.44 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

    此方案可获得 ≥ 0.38 mg/mL (0.79 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 3.8 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

  • 3.

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

    Solubility: ≥ 0.38 mg/mL (0.79 mM); Clear solution

    此方案可获得 ≥ 0.38 mg/mL (0.79 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 3.8 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]. Sakamoto H, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011, 19(5), 679-690.

    [2]. Gadgeel S, et al. Alectinib versus crizotinib in treatment-naive anaplastic lymphoma kinase-positive (ALK+) non-small-cell lung cancer: CNS efficacy results from the ALEX study. Ann Oncol. 2018 Nov 1;29(11):2214-2222.

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