ALK inhibitor 1

发表于2024年4月13日由上海金畔生物科技有限公司

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。

ALK inhibitor 1 纯度: 99.71%

ALK inhibitor 1 (compound 17) 是一种有效的，嘧啶类 ALK 抑制剂。ALK inhibitor 1 是有效的睾丸特异性丝氨酸/苏氨酸激酶 2 (TSSK2; IC₅₀=31 nM) 和粘着斑激酶 (FAK; IC₅₀=2 nM) 抑制剂。

ALK inhibitor 1 Chemical Structure

CAS No. : 761436-81-1

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥2722	In-stock
2 mg	￥1460	In-stock
5 mg	￥2200	In-stock
10 mg	￥3329	In-stock
25 mg	￥6900	In-stock
50 mg	￥11000	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

ALK inhibitor 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Cytoskeleton Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library

生物活性

ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC₅₀=31 nM) and focal adhesion kinase (FAK; IC₅₀=2 nM)^[1].

体外研究
(In Vitro)

ALK inhibitor 1 (compound 17) inhibits IGF-1R with an IC₅₀ of 90 nM^[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

562.48

Formula

C₂₃H₂₈BrN₇O₃S

CAS 号

761436-81-1

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 : ≥ 100 mg/mL (177.78 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	1.7778 mL	8.8892 mL	17.7784 mL
5 mM	0.3556 mL	1.7778 mL	3.5557 mL
10 mM	0.1778 mL	0.8889 mL	1.7778 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 (4.44 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.44 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% corn oil

Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.44 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]. Jon E Hawkinson, et al. Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis-Specific Serine/Threonine Kinase 2 (TSSK2). ChemMedChem. 2017 Nov 22;12(22):1857-1865.

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ALK-IN-1(Synonyms: Brigatinib analog)

发表于2024年4月10日由上海金畔生物科技有限公司

ALK-IN-1 (Synonyms: Brigatinib analog) 纯度: 99.94%

ALK-IN-1 (Brigatinib analog) 是 ALK 激酶高效选择性抑制剂，出自专利 US20140066406 A1。

ALK-IN-1 Chemical Structure

CAS No. : 1197958-12-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥931	In-stock
2 mg	￥600	In-stock
5 mg	￥800	In-stock
10 mg	￥1400	In-stock
50 mg	￥3500	In-stock
100 mg	￥4500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

ALK-IN-1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Blood Cancer Compound Library

生物活性

ALK-IN-1 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.

分子量

529.01

Formula

C₂₆H₃₄ClN₆O₂P

CAS 号

1197958-12-5

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 (94.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8903 mL	9.4516 mL	18.9032 mL
5 mM	0.3781 mL	1.8903 mL	3.7806 mL
10 mM	0.1890 mL	0.9452 mL	1.8903 mL

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：

1.

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

Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.73 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 (4.73 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.73 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 (4.73 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.73 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]. Sen Zhang, Frank Wang, Jeffrey Keats, Abstract LB-298: AP26113, a potent ALK inhibitor, overcomes mutations in EML4-ALK that confer resistance to PF-02341066 (PF1066). Cancer Research: April 15, 2010; Volume 70, Issue 8, Supplement 1

[2]. Victor M. Rivera, Frank Wang, Rana Anjum, Abstract 1794: AP26113 is a dual ALK/EGFR inhibitor: Characterization against EGFR T790M in cell and mouse models of NSCLC. Cancer Research: April 15, 2012; Volume 72, Issue 8, Supplement 1

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

MS4077

发表于2024年3月19日由上海金畔生物科技有限公司

MS4077 纯度: 99.49%

MS4077 是基于 Cereblon 配体的间变性淋巴瘤激酶 (ALK) PROTAC (降解物)，结合 ALK, K_d 为 37 nM。

MS4077 Chemical Structure

CAS No. : 2230077-10-6

规格	价格	是否有货
1 mg	￥3500	In-stock
5 mg	￥10500	In-stock
10 mg		询价
50 mg		询价

* Please select Quantity before adding items.

MS4077 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a K_d of 37 nM for binding affinity to ALK^[1].

IC₅₀ & Target

ALK

Cereblon

体外研究
(In Vitro)

MS4077 effectively inhibits cancer cell proliferation. MS4077 (10^-3-1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1 cells with an IC₅₀ of 46 ± 4 nM. In comparison with SU-DHL-1 cells, the proliferation of NCI-H2228 cells is less sensitive to MS4077(10^-2-10^0.5 μM; 3 days)^[1].
MS4077 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228 cells in a concentration-dependent manner. In SU-DHL-1 cells, MS4077 reduces the NPM-ALK protein levels with impressive DC₅₀ (50% degradation) value of 3±1 nM after 16-hour treatment. Over 90% of inhibition of both ALK Y1507 and STAT3 Y705 phosphorylation is achieved at the 100 nM concentration. In NCI-H2228 cells, MS4077 reduces the EML4-ALK protein levels with similar DC₅₀ value of 34±9 nM after 16-hour treatment. At the 100 nM concentration, NCI-H2228 cells reduces more than 90% of EML4-ALK protein levels^[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.

Cell Viability Assay^[1]

Cell Line:	SU-DHL-1 and NCI-H2228 cells
Concentration:	10^-3, 10^-2.5, 10^-2,10^-1.5, 10^-1, 10^-0.5, and 1 μM for SU-DHL-1  cells; 10^-2, 10^-1.5, 10^-1, 10^-0.5, 1, 10^0.5 μM for NCI-H2228 cells
Incubation Time:	3 days
Result:	Inhibited proliferation of SU-DHL-1 cells (IC₅₀=46 ± 4 nM). Less sensitive to the proliferation of NCI-H2228 cells than SU-DHL-1 cells.

Western Blot Analysis^[1]

Cell Line:	SU-DHL-1 and NCI-H2228 cells
Concentration:	1, 3, 10, 30, and 100 μM for SU-DHL-1 cells; 3, 10, 30, 60, and 100 μM for NCI-H2228 cells
Incubation Time:	16 hours
Result:	Reduced the NPM-ALK protein levels with impressive DC₅₀ of  3 ± 1 nM in SU-DHL-1 cells. Reduced the EML4-ALK protein levels with similar DC₅₀ of 34 ± 9 nM in NCI-H2228 cells.

分子量

1134.73

Formula

C₅₅H₇₂ClN₉O₁₃S

CAS 号

2230077-10-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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 : 110 mg/mL (96.94 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.8813 mL	4.4063 mL	8.8127 mL
5 mM	0.1763 mL	0.8813 mL	1.7625 mL
10 mM	0.0881 mL	0.4406 mL	0.8813 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。

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：

1.

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

Solubility: 6 mg/mL (5.29 mM); Suspended solution; Need ultrasonic

此方案可获得 6 mg/mL (5.29 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 60.0 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: ≥ 6 mg/mL (5.29 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (5.29 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 60.0 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

*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]. Zhang C, et al. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). Eur J Med Chem. 2018 May 10;151:304-314.

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

ALK inhibitor 2

发表于2024年3月9日由上海金畔生物科技有限公司

ALK inhibitor 2 纯度: 99.77%

ALK inhibitor 2 (compound 18) 是一种有效的，嘧啶类 ALK 抑制剂。ALK inhibitor 2 是有效的睾丸特异性丝氨酸/苏氨酸激酶 2 (TSSK2; IC₅₀=37 nM) 和粘着斑激酶 (FAK; IC₅₀=5 nM) 抑制剂。

ALK inhibitor 2 Chemical Structure

CAS No. : 761438-38-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2714	In-stock
5 mg	￥2381	In-stock
10 mg	￥3329	In-stock
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

ALK inhibitor 2 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Cytoskeleton Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library

生物活性

ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC₅₀=37 nM) and focal adhesion kinase (FAK; IC₅₀=5 nM)^[1].

IC₅₀ & Target

IC50: 37 nM (TSSK2) and 5 nM (FAK)^[1]

体外研究
(In Vitro)

Testis-specific serine/threonine kinase 2 (TSSK2) is an important target for reversible male contraception. ALK inhibitor 2 (compound 18) contains a methylpiperazine A ring (R1=Me, X=N) and a D ring with R5=methylsulfonamide. ALK inhibitor 2 can undergo metabolic oxidation to form reactive adducts in the presence of glutathione^[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

518.03

Formula

C₂₃H₂₈ClN₇O₃S

CAS 号

761438-38-4

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 (96.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9304 mL	9.6519 mL	19.3039 mL
5 mM	0.3861 mL	1.9304 mL	3.8608 mL
10 mM	0.1930 mL	0.9652 mL	1.9304 mL

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：

1.

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

Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.83 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% corn oil

Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.83 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]. Jon E Hawkinson, et al. Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis-Specific Serine/Threonine Kinase 2 (TSSK2). ChemMedChem. 2017 Nov 22;12(22):1857-1865.

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

IN-1130

发表于2024年3月6日由上海金畔生物科技有限公司

IN-1130 纯度: 99.79%

N-1130 是一种高度选择性的转化生长因子-β I 型受体激酶 (ALK5) 抑制剂，对 ALK5 介导的 Smad3 磷酸化的 IC₅₀ 为 5.3 nM。IN-1130 抑制酪蛋白的 ALK5 磷酸化 (IC₅₀=36 nM)，抑制 p38α 丝裂原活化的蛋白激酶 (IC₅₀=4.3 μM)。IN-1130 可抑制阻塞性肾病中的肾纤维化，阻止乳腺癌的肺转移。

IN-1130 Chemical Structure

CAS No. : 868612-83-3

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1100	In-stock
5 mg	￥1000	In-stock
10 mg	￥1700	In-stock
25 mg	￥3500	In-stock
50 mg	￥5500	In-stock
100 mg	￥9500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

IN-1130 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
TGF-beta/Smad Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Breast Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Angiogenesis Related Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library
Anti-Colorectal Cancer Compound Library

生物活性

IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC₅₀ of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC₅₀=36 nM) and p38α mitogen-activated protein kinase (IC₅₀=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis^[1]^[2].

IC₅₀ & Target^[1]

ALK5

体外研究
(In Vitro)

IN-1130 (0.5, 1 μM; for 2 hours) inhibits TGF-β-stimulated Smad2 phosphorylation and subsequent nuclear translocation in HepG2 and 4T1 cells^[2].
IN-1130 (1 μM; for 72 hours) restores the TGF-β-mediated decrease in E-cadherin protein expression. IN-1130 (1 μM; for 72 hours) inhibits TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs in MCF10A cells^[2].
IN-1130 (1 μM; pretreated for 30 min) inhibits TGF-β-induced MDA-MB-231 cells, NMuMG, and MCF10A cells mobility and invasion^[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.

Western Blot Analysis^[2]

Cell Line:	HepG2 and 4T1 cells
Concentration:	0.5, 1 μM
Incubation Time:	For 2 hours
Result:	Inhibited TGF-β-stimulated Smad2 phosphorylation.

RT-PCR^[2]

Cell Line:	MCF10A cells
Concentration:	1 μM
Incubation Time:	For 72 hours
Result:	Inhibited TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs.

体内研究
(In Vivo)

IN-1130 (10, 20 mg/kg/day; IP; for 7 and 14 days) reduces the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg and significantly reduces or absent histopathological changes with 20 mg/kg in unilateral ureteral obstruction (UUO) rats^[1].
IN-1130 (10, 20 mg/kg/day; for 14 days) dose-dependently decreases levels of TGF-β1 mRNA and suppresses phosphorylation of Smad2, α-SMA, myofibroblasts in rat UUO kidneys^[1].
IN-1130 (40 mg/kg; IP; 3 times per week for 3 weeks) inhibits in vivo breast cancer metastasis to the lungs in MMTV/c-Neu mice (Eight-week-old female BALB/c 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.

Animal Model:	Six-week-old male Sprague–Dawley rats weighing 180-200 g^[1]
Dosage:	10 and 20 mg/kg
Administration:	IP; daily; for 7 and 14 days
Result:	Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg.

分子量

420.47

Formula

C₂₅H₂₀N₆O

CAS 号

868612-83-3

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 : 100 mg/mL (237.83 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3783 mL	11.8915 mL	23.7829 mL
5 mM	0.4757 mL	2.3783 mL	4.7566 mL
10 mM	0.2378 mL	1.1891 mL	2.3783 mL

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：

1.

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

Solubility: ≥ 1.43 mg/mL (3.40 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (3.40 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 14.3 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

*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]. Moon JA, et al. IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 2006 Oct;70(7):1234-43.

[2]. Park CY, et al. An novel inhibitor of TGF-β type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 2014 Aug 28;351(1):72-80.

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ALK2-IN-2

发表于2024年2月27日由上海金畔生物科技有限公司

ALK2-IN-2 纯度: 99.90%

ALK2-IN-2 是一种有效的、选择性的活化素受体样激酶 2 (ALK2) 抑制剂，IC₅₀ 值为 9 nM，对 ALK2 的抑制作用是 ALK3 的 700 倍。

ALK2-IN-2 Chemical Structure

CAS No. : 2254409-25-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3832	In-stock
5 mg	￥3500	In-stock
10 mg	￥5500	In-stock
25 mg	￥9900	In-stock
50 mg	￥16500	In-stock
100 mg	￥22500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

ALK2-IN-2 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
TGF-beta/Smad Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Pancreatic Cancer Compound Library
Angiogenesis Related Compound Library
Targeted Diversity Library
Anti-Colorectal Cancer Compound Library

生物活性

ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC₅₀ of 9 nM, and over 700-fold selectivity against ALK3^[1].

IC₅₀ & Target

ALK2

9 nM (IC₅₀)

分子量

497.61

Formula

C₂₈H₂₇N₅O₂S

CAS 号

2254409-25-9

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 : 125 mg/mL (251.20 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0096 mL	10.0480 mL	20.0961 mL
5 mM	0.4019 mL	2.0096 mL	4.0192 mL
10 mM	0.2010 mL	1.0048 mL	2.0096 mL

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：

1.

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

Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.18 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 (4.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.18 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.18 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]. Jiang JK, et al. Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors. Bioorg Med Chem Lett. 2018 Nov 1;28(20):3356-3362.

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SIAIS164018

发表于2024年2月27日由上海金畔生物科技有限公司

SIAIS164018

SIAIS164018 是一种基于 PROTAC 的 ALK 和 EGFR 降解剂，由 Brigatinib 设计，对 ALK 和 ALK G1202R 的 IC₅₀ 分别为 2.5 nM 和 6.6 nM。SIAIS164018 强烈抑制癌细胞迁移和侵袭，引起细胞阻滞在 G1 期，诱导细胞凋亡 (apoptosis)。SIAIS164018表现出比 Brigatinib 更好的性能。

SIAIS164018 Chemical Structure

CAS No. : 2353492-68-7

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	SIAIS164018 is a PROTAC-based ALK and EGFR degrader, which is designed from Brigatinib, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib^[1].
IC₅₀ & Target	IC₅₀: 2.5 nM (ALK), 6.6 nM (ALK G1202R)^[1]
体外研究 (In Vitro)	SIAIS164018 significantly inhibits SR cell proliferation with an IC₅₀ value of 2 nM^[1]. SIAIS164018 shows better cell proliferation inhibition than Brigatinib does in ALK (G1202R) over-expressing 293T and EGFR expressing H1975 cell lines with IC₅₀s 21 and 42 nM, respectively^[1]. SIAIS164018 (100 nM; 24 or 48 h) induces a significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	883.33
Formula	C₄₃H₄₈ClN₁₀O₇P
CAS 号	2353492-68-7
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]. Ren C, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. J Med Chem. 2021 Jul 8;64(13):9152-9165.

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ZX-29

发表于2024年1月19日由上海金畔生物科技有限公司

ZX-29 纯度: 99.52%

ZX-29 是一种有效的选择性的 ALK 抑制剂，对 ALK，ALK L1196M 和 ALK G1202R 的 IC₅₀ 分别为 2.1 nM，1.3 nM 和 3.9 nM，但对 EGFR 无活性。ZX-29 通过诱导内质网应激来诱导细胞凋亡 (apoptosis)，并克服了由 ALK 突变引起的细胞抗性。ZX-29 还可诱导保护性自噬 (autophagy) 并具有抗肿瘤作用。

ZX-29 Chemical Structure

CAS No. : 2254805-62-2

规格	价格	是否有货
5 mg	￥3000	In-stock
10 mg	￥4800	In-stock
25 mg	￥9500	In-stock
50 mg	￥14500	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

ZX-29 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library
Endoplasmic Reticulum Stress Compound Library
Anti-Lung Cancer Compound Library

生物活性

ZX-29 is a potent and selective ALK inhibitor with an IC₅₀ of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect^[1].

IC₅₀ & Target

IC50: 2.1 nM (ALK), 1.3 nM (ALK L1196M) and 3.9 nM (ALK G1202R)^[1]

体外研究
(In Vitro)

ZX-29 (0-81 nM; 24-72 hours; NCI-H2228 cells) treatment leads to a time- and dose-dependent decrease in NCI-H2228 cell viability^[1].
ZX-29 (10 nM; 24 hours; NCI-H2228 cells) treatment causes typical signs of autophagy and the formation of autophagosomes. ZX-29 enhances the expression level of LC3 and Beclin1^[1].
ZX-29 (10 nM; 0-48 hours; NCI-H2228 cells) inhibits the proliferation of NCI-H2228 cells and arrests the cells in G1 phase^[1].
ZX-29 (10-40 nM; 24-48 hours; NCI-H2228 cells) treatment induces apoptosis of NCI-H2228 cells. ZX-29 dose-dependently upregulates the expression levels of proapoptotic protein Bax, increases the production of activated forms of caspase 3, and downregulates the expression level of antiapoptotic protein Bcl-2^[1].
ZX-29 (30-300 nM; 24 hours; NCI-H2228 cells) treatment significantly down-regulates the expression of p-ALK and its downstream signaling proteins, including p-Akt and p-STAT3, in a dose-dependent manner^[1].
ZX-29 (20 nM; 0-48 hours; NCI-H2228 cells) treatment significantly increases the mRNA level of CHOP^[1].
ZX-29 dose-dependently inhibits colony formation of NCI-H2228 cells. With an increase in ZX-29 concentration, the cell density decreased gradually, and the cells lost their normal morphology and become sharp and slender^[1].

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

Cell Viability Assay^[1]

Cell Line:	NCI-H2228 cells
Concentration:	0 nM, 1 nM, 3 nM, 9 nM, 10 nM, 27 nM or 81 nM
Incubation Time:	24 hours, 48 hours or 72 hours
Result:	Led to a time- and dose-dependent decrease in NCI-H2228 cell viability.

Cell Autophagy Assay^[1]

Cell Line:	NCI-H2228 cells
Concentration:	10 nM
Incubation Time:	24 hours
Result:	Caused typical signs of autophagy and the formation of autophagosomes.

Cell Cycle Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	0 hour, 12 hours, 24 hours or 48 hours
Incubation Time:	24 hours
Result:	Arrested the NCI-H2228 cells in G1 phase in a time-dependent manner.

Apoptosis Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	10 nM, 20 nM or 40 nM
Incubation Time:	24 hours, 48 hours
Result:	Promoted NCI-H2228 cell apoptosis in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	30 nM, 100 nM, 300 nM
Incubation Time:	24 hours
Result:	Significantly down-regulated the expression of p-ALK and its downstream signaling proteins, including p-Akt and p-STAT3, in a dose-dependent manner.

RT-PCR^[1]

Cell Line:	NCI-H2228 cells
Concentration:	20 nM
Incubation Time:	0 hour, 6 hours, 12 hours, 24 hours or 48 hours
Result:	The mRNA level of CHOP was increased significantly.

体内研究
(In Vivo)

ZX-29 (50 mg/kg; intragastric administration; every 2 days; for a total of 7 times; female BALB/c nude mice) treatment suppresses tumor growth in a mouse xenograft model^[1].

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

Animal Model:	Female BALB/c nude mice (4-week-old) with H2228 cells^[1]
Dosage:	50 mg/kg
Administration:	Intragastric administration; every 2 days; for a total of 7 times
Result:	Showed significantly attenuated tumor growth.

分子量

518.03

Formula

C₂₃H₂₈ClN₇O₃S

CAS 号

2254805-62-2

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 : 50 mg/mL (96.52 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	1.9304 mL	9.6519 mL	19.3039 mL
5 mM	0.3861 mL	1.9304 mL	3.8608 mL
10 mM	0.1930 mL	0.9652 mL	1.9304 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：

1.

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

Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.83 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

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Gou W, et al. ZX-29, a novel ALK inhibitor, induces apoptosis via ER stress in ALK rearrangement NSCLC cells and overcomes cell resistance caused by an ALK mutation. Biochim Biophys Acta Mol Cell Res. 2020 Mar 26;1867(7):118712.

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ZX-29

发表于2024年1月19日由上海金畔生物科技有限公司

ZX-29 纯度: 99.52%

ZX-29 Chemical Structure

CAS No. : 2254805-62-2

规格	价格	是否有货
5 mg	￥3000	In-stock
10 mg	￥4800	In-stock
25 mg	￥9500	In-stock
50 mg	￥14500	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

ZX-29 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library
Endoplasmic Reticulum Stress Compound Library
Anti-Lung Cancer Compound Library

生物活性

IC₅₀ & Target

IC50: 2.1 nM (ALK), 1.3 nM (ALK L1196M) and 3.9 nM (ALK G1202R)^[1]

体外研究
(In Vitro)

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.

Cell Viability Assay^[1]

Cell Line:	NCI-H2228 cells
Concentration:	0 nM, 1 nM, 3 nM, 9 nM, 10 nM, 27 nM or 81 nM
Incubation Time:	24 hours, 48 hours or 72 hours
Result:	Led to a time- and dose-dependent decrease in NCI-H2228 cell viability.

Cell Autophagy Assay^[1]

Cell Line:	NCI-H2228 cells
Concentration:	10 nM
Incubation Time:	24 hours
Result:	Caused typical signs of autophagy and the formation of autophagosomes.

Cell Cycle Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	0 hour, 12 hours, 24 hours or 48 hours
Incubation Time:	24 hours
Result:	Arrested the NCI-H2228 cells in G1 phase in a time-dependent manner.

Apoptosis Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	10 nM, 20 nM or 40 nM
Incubation Time:	24 hours, 48 hours
Result:	Promoted NCI-H2228 cell apoptosis in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	30 nM, 100 nM, 300 nM
Incubation Time:	24 hours
Result:	Significantly down-regulated the expression of p-ALK and its downstream signaling proteins, including p-Akt and p-STAT3, in a dose-dependent manner.

RT-PCR^[1]

Cell Line:	NCI-H2228 cells
Concentration:	20 nM
Incubation Time:	0 hour, 6 hours, 12 hours, 24 hours or 48 hours
Result:	The mRNA level of CHOP was increased significantly.

体内研究
(In Vivo)

ZX-29 (50 mg/kg; intragastric administration; every 2 days; for a total of 7 times; female BALB/c nude mice) treatment suppresses tumor growth in a mouse xenograft 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:	Female BALB/c nude mice (4-week-old) with H2228 cells^[1]
Dosage:	50 mg/kg
Administration:	Intragastric administration; every 2 days; for a total of 7 times
Result:	Showed significantly attenuated tumor growth.

分子量

518.03

Formula

C₂₃H₂₈ClN₇O₃S

CAS 号

2254805-62-2

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 : 50 mg/mL (96.52 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	1.9304 mL	9.6519 mL	19.3039 mL
5 mM	0.3861 mL	1.9304 mL	3.8608 mL
10 mM	0.1930 mL	0.9652 mL	1.9304 mL

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：

1.

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

Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.83 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

*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]. Gou W, et al. ZX-29, a novel ALK inhibitor, induces apoptosis via ER stress in ALK rearrangement NSCLC cells and overcomes cell resistance caused by an ALK mutation. Biochim Biophys Acta Mol Cell Res. 2020 Mar 26;1867(7):118712.

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

ZX-29

发表于2024年1月19日由上海金畔生物科技有限公司

ZX-29 纯度: 99.52%

ZX-29 Chemical Structure

CAS No. : 2254805-62-2

规格	价格	是否有货
5 mg	￥3000	In-stock
10 mg	￥4800	In-stock
25 mg	￥9500	In-stock
50 mg	￥14500	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

ZX-29 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library
Endoplasmic Reticulum Stress Compound Library
Anti-Lung Cancer Compound Library

生物活性

IC₅₀ & Target

IC50: 2.1 nM (ALK), 1.3 nM (ALK L1196M) and 3.9 nM (ALK G1202R)^[1]

体外研究
(In Vitro)

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

Cell Viability Assay^[1]

Cell Line:	NCI-H2228 cells
Concentration:	0 nM, 1 nM, 3 nM, 9 nM, 10 nM, 27 nM or 81 nM
Incubation Time:	24 hours, 48 hours or 72 hours
Result:	Led to a time- and dose-dependent decrease in NCI-H2228 cell viability.

Cell Autophagy Assay^[1]

Cell Line:	NCI-H2228 cells
Concentration:	10 nM
Incubation Time:	24 hours
Result:	Caused typical signs of autophagy and the formation of autophagosomes.

Cell Cycle Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	0 hour, 12 hours, 24 hours or 48 hours
Incubation Time:	24 hours
Result:	Arrested the NCI-H2228 cells in G1 phase in a time-dependent manner.

Apoptosis Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	10 nM, 20 nM or 40 nM
Incubation Time:	24 hours, 48 hours
Result:	Promoted NCI-H2228 cell apoptosis in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:	NCI-H2228 cells
Concentration:	30 nM, 100 nM, 300 nM
Incubation Time:	24 hours
Result:	Significantly down-regulated the expression of p-ALK and its downstream signaling proteins, including p-Akt and p-STAT3, in a dose-dependent manner.

RT-PCR^[1]

Cell Line:	NCI-H2228 cells
Concentration:	20 nM
Incubation Time:	0 hour, 6 hours, 12 hours, 24 hours or 48 hours
Result:	The mRNA level of CHOP was increased significantly.

体内研究
(In Vivo)

ZX-29 (50 mg/kg; intragastric administration; every 2 days; for a total of 7 times; female BALB/c nude mice) treatment suppresses tumor growth in a mouse xenograft model^[1].

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

Animal Model:	Female BALB/c nude mice (4-week-old) with H2228 cells^[1]
Dosage:	50 mg/kg
Administration:	Intragastric administration; every 2 days; for a total of 7 times
Result:	Showed significantly attenuated tumor growth.

分子量

518.03

Formula

C₂₃H₂₈ClN₇O₃S

CAS 号

2254805-62-2

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 : 50 mg/mL (96.52 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	1.9304 mL	9.6519 mL	19.3039 mL
5 mM	0.3861 mL	1.9304 mL	3.8608 mL
10 mM	0.1930 mL	0.9652 mL	1.9304 mL

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：

1.

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

Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.83 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

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Gou W, et al. ZX-29, a novel ALK inhibitor, induces apoptosis via ER stress in ALK rearrangement NSCLC cells and overcomes cell resistance caused by an ALK mutation. Biochim Biophys Acta Mol Cell Res. 2020 Mar 26;1867(7):118712.

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ALK/ROS1-IN-1

发表于2024年1月18日由上海金畔生物科技有限公司

ALK/ROS1-IN-1

ALK/ROS1-IN-1 (compound 2e) 是一种高效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂，对 ALK 和 ROS1 酶作用的 IC₅₀ 值分别为 0.174 μM 和 0.530 μM。

ALK/ROS1-IN-1 Chemical Structure

CAS No. : 2365497-07-8

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	ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC₅₀s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
IC₅₀ & Target	IC50: 0.174 μM (ALK), 0.530 μM (ROS1)^[1]
体外研究 (In Vitro)	ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC₅₀= 6.27 μM and 10.71 μM, respectively)^[1]. ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALK^L1196M with an IC₅₀ value of 41.3 nM^[1]. ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC₅₀s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively^[1]. ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	584.63
Formula	C₃₀H₃₅F₃N₆O₃
CAS 号	2365497-07-8
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]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375.

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ALK/ROS1-IN-1

发表于2024年1月18日由上海金畔生物科技有限公司

ALK/ROS1-IN-1

ALK/ROS1-IN-1 (compound 2e) 是一种高效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂，对 ALK 和 ROS1 酶作用的 IC₅₀ 值分别为 0.174 μM 和 0.530 μM。

ALK/ROS1-IN-1 Chemical Structure

CAS No. : 2365497-07-8

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	ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC₅₀s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
IC₅₀ & Target	IC50: 0.174 μM (ALK), 0.530 μM (ROS1)^[1]
体外研究 (In Vitro)	ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC₅₀= 6.27 μM and 10.71 μM, respectively)^[1]. ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALK^L1196M with an IC₅₀ value of 41.3 nM^[1]. ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC₅₀s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively^[1]. ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line^[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	584.63
Formula	C₃₀H₃₅F₃N₆O₃
CAS 号	2365497-07-8
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]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375.

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

ALK/ROS1-IN-1

发表于2024年1月18日由上海金畔生物科技有限公司

ALK/ROS1-IN-1

ALK/ROS1-IN-1 (compound 2e) 是一种高效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂，对 ALK 和 ROS1 酶作用的 IC₅₀ 值分别为 0.174 μM 和 0.530 μM。

ALK/ROS1-IN-1 Chemical Structure

CAS No. : 2365497-07-8

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	ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC₅₀s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
IC₅₀ & Target	IC50: 0.174 μM (ALK), 0.530 μM (ROS1)^[1]
体外研究 (In Vitro)	ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC₅₀= 6.27 μM and 10.71 μM, respectively)^[1]. ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALK^L1196M with an IC₅₀ value of 41.3 nM^[1]. ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC₅₀s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively^[1]. ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	584.63
Formula	C₃₀H₃₅F₃N₆O₃
CAS 号	2365497-07-8
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]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375.

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

ALK-IN-13

发表于2023年12月19日由上海金畔生物科技有限公司

ALK-IN-13

ALK-IN-13 是一种 ALK 抑制剂，来自专利 US20130225528A1，example 19。

ALK-IN-13 Chemical Structure

CAS No. : 1197953-88-0

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	ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19^[1].
分子量	584.09
Formula	C₂₉H₃₉ClN₇O₂P
CAS 号	1197953-88-0
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]. Yihan Wang, et al. Phosphorus Derivatives as Kinase Inhibitors. US20130225528A1.

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

ALK-IN-13

发表于2023年12月19日由上海金畔生物科技有限公司

ALK-IN-13

ALK-IN-13 是一种 ALK 抑制剂，来自专利 US20130225528A1，example 19。

ALK-IN-13 Chemical Structure

CAS No. : 1197953-88-0

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	ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19^[1].
分子量	584.09
Formula	C₂₉H₃₉ClN₇O₂P
CAS 号	1197953-88-0
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]. Yihan Wang, et al. Phosphorus Derivatives as Kinase Inhibitors. US20130225528A1.

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

ALK-IN-13

发表于2023年12月19日由上海金畔生物科技有限公司

ALK-IN-13

ALK-IN-13 是一种 ALK 抑制剂，来自专利 US20130225528A1，example 19。

ALK-IN-13 Chemical Structure

CAS No. : 1197953-88-0

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	ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19^[1].
分子量	584.09
Formula	C₂₉H₃₉ClN₇O₂P
CAS 号	1197953-88-0
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]. Yihan Wang, et al. Phosphorus Derivatives as Kinase Inhibitors. US20130225528A1.

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

ALK-IN-12

发表于2023年12月18日由上海金畔生物科技有限公司

ALK-IN-12

ALK-IN-12 是一种有效且具有口服活性的 ALK 抑制剂，IC₅₀ 为 0.18 nM。ALK-IN-12 还抑制 IGF1R 和 InsR (IC₅₀=20.3 和 90.6 nM)。具有抗肿瘤活性。

ALK-IN-12 Chemical Structure

CAS No. : 1197958-53-4

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

ALK-IN-12 is a potent and orally active ALK inhibitor with an IC₅₀ of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC₅₀=20.3 and 90.6 nM). Antitumor activities^[1].

体外研究
(In Vitro)

ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC₅₀ of 28.3 nM^[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)

ALK-IN-12 (10-50 mg/kg; orally; once daily for 13 consecutive days) shows dose-dependent antitumor activity^[1].
ALK-IN-12 (3 mg/kg; i.v.; 6-8 week old female CD rats ) treatment shows AUC_0-∞, CL, t_1/2 and V_ss are 3039 ng•h/mL, 0.91 h•kg, 6.6 hours and 6.12 L/kg, respectively^[1].
ALK-IN-12 (10 mg/kg; p.o.; 6-8 week old female CD rats) treatment shows C_max, AUC_0-∞, t_max, t_1/2 and F are 3254 ng/mL, 4056 ng•h/mL, 6.0 hours, 12.5 hours and 39%, respectively^[1].

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

Animal Model:	Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)^[1]
Dosage:	10-50 mg/kg
Administration:	Orally; once daily for 13 consecutive days
Result:	Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose).

分子量

500.96

Formula

C₂₄H₃₀ClN₆O₂P

CAS 号

1197958-53-4

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]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016;59(10):4948-4964.

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

ALK-IN-12

发表于2023年12月18日由上海金畔生物科技有限公司

ALK-IN-12

ALK-IN-12 是一种有效且具有口服活性的 ALK 抑制剂，IC₅₀ 为 0.18 nM。ALK-IN-12 还抑制 IGF1R 和 InsR (IC₅₀=20.3 和 90.6 nM)。具有抗肿瘤活性。

ALK-IN-12 Chemical Structure

CAS No. : 1197958-53-4

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

ALK-IN-12 is a potent and orally active ALK inhibitor with an IC₅₀ of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC₅₀=20.3 and 90.6 nM). Antitumor activities^[1].

体外研究
(In Vitro)

ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC₅₀ of 28.3 nM^[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)

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

Animal Model:	Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)^[1]
Dosage:	10-50 mg/kg
Administration:	Orally; once daily for 13 consecutive days
Result:	Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose).

分子量

500.96

Formula

C₂₄H₃₀ClN₆O₂P

CAS 号

1197958-53-4

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]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016;59(10):4948-4964.

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

ALK-IN-12

发表于2023年12月18日由上海金畔生物科技有限公司

ALK-IN-12

ALK-IN-12 是一种有效且具有口服活性的 ALK 抑制剂，IC₅₀ 为 0.18 nM。ALK-IN-12 还抑制 IGF1R 和 InsR (IC₅₀=20.3 和 90.6 nM)。具有抗肿瘤活性。

ALK-IN-12 Chemical Structure

CAS No. : 1197958-53-4

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

ALK-IN-12 is a potent and orally active ALK inhibitor with an IC₅₀ of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC₅₀=20.3 and 90.6 nM). Antitumor activities^[1].

体外研究
(In Vitro)

ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC₅₀ of 28.3 nM^[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)

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:	Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)^[1]
Dosage:	10-50 mg/kg
Administration:	Orally; once daily for 13 consecutive days
Result:	Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose).

分子量

500.96

Formula

C₂₄H₃₀ClN₆O₂P

CAS 号

1197958-53-4

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]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016;59(10):4948-4964.

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

ALK kinase inhibitor-1

发表于2023年12月13日由上海金畔生物科技有限公司

ALK kinase inhibitor-1 纯度: 99.85%

ALK kinase inhibitor-1 是一种间变性淋巴瘤激酶 ALK 抑制剂，详细信息请参考专利文献 US20130261106A1 中的化合物 I-202。

ALK kinase inhibitor-1 Chemical Structure

CAS No. : 1462949-64-9

规格	价格	是否有货
5 mg	￥500	In-stock
10 mg	￥720	In-stock
50 mg	￥1950	In-stock
100 mg	￥2950	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

ALK kinase inhibitor-1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Blood Cancer Compound Library

生物活性

ALK kinase inhibitor-1 is an anaplastic lymphoma kinase (ALK) inhibitor extracted from patent US20130261106A1 compound I-202^[1].

分子量

537.65

Formula

C₂₈H₃₂FN₅O₃S

CAS 号

1462949-64-9

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 : 100 mg/mL (185.99 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8599 mL	9.2997 mL	18.5995 mL
5 mM	0.3720 mL	1.8599 mL	3.7199 mL
10 mM	0.1860 mL	0.9300 mL	1.8599 mL

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：

1.

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

Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.65 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

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。

参考文献

[1]. Carry JC, et, al. Novel thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof. US20130261106A1.

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