标签归档：flt

FLT3-IN-12

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。

FLT3-IN-12 

FLT3-IN-12 是一种有效的、选择性的、具有口服活性的 FLT3 激酶抑制剂，对 FLT3-WT 和 FLT3-D835Y 的 IC50 分别为 1.48 nM 和 2.87 nM。FLT3-IN-12 具有比 c-KIT 高的选择性 (>1000 倍)。FLT3-IN-12 具有出色的抗急性髓性白血病活性 (MV4-11细胞，IC50 为 0.75 nM)。

FLT3-IN-12

FLT3-IN-12 Chemical Structure

CAS No. : 2499966-67-3

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

FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM)[1].

IC50 & Target

IC50: 1.48 nM (FLT3-WT) and 2.87 nM (FLT3-D835Y)[1]
体外研究
(In Vitro)

FLT3-IN-12 (compound 36) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y with the IC50 range is 0.16-14.5 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)

Oral administration of FLT3-IN-12 (compound 36) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting a tumor growth inhibitory rate of 95.1%. Importantly, FLT3-IN-12 could prolong the mouse survival time in the FLT3-ITD-TKD dual mutation syngeneic mouse model (BaF3-FLT3-ITD-D835Y) at a dose of 6 mg/kg p.o. bid/4W[1].
FLT3-IN-12 (compound 36; 20 mg/kg; oral administration) exhibits excellent plasma exposure (area under the curve (AUC)0–∞ of 5278 ng·h/mL), T1/2 of 3.7 hours, and high maximum plasma concentrations (Cmax of 775 ng/mL)[1].

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

432.44

Formula

C21H23F3N6O
CAS 号

2499966-67-3
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]. Lexian Tong, et al. Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. J Med Chem. 2022 Feb 24;65(4):3229-3248.

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

FLT3-IN-12

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。

FLT3-IN-12 

FLT3-IN-12 是一种有效的、选择性的、具有口服活性的 FLT3 激酶抑制剂，对 FLT3-WT 和 FLT3-D835Y 的 IC50 分别为 1.48 nM 和 2.87 nM。FLT3-IN-12 具有比 c-KIT 高的选择性 (>1000 倍)。FLT3-IN-12 具有出色的抗急性髓性白血病活性 (MV4-11细胞，IC50 为 0.75 nM)。

FLT3-IN-12

FLT3-IN-12 Chemical Structure

CAS No. : 2499966-67-3

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

FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM)[1].

IC50 & Target

IC50: 1.48 nM (FLT3-WT) and 2.87 nM (FLT3-D835Y)[1]
体外研究
(In Vitro)

FLT3-IN-12 (compound 36) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y with the IC50 range is 0.16-14.5 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)

Oral administration of FLT3-IN-12 (compound 36) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting a tumor growth inhibitory rate of 95.1%. Importantly, FLT3-IN-12 could prolong the mouse survival time in the FLT3-ITD-TKD dual mutation syngeneic mouse model (BaF3-FLT3-ITD-D835Y) at a dose of 6 mg/kg p.o. bid/4W[1].
FLT3-IN-12 (compound 36; 20 mg/kg; oral administration) exhibits excellent plasma exposure (area under the curve (AUC)0–∞ of 5278 ng·h/mL), T1/2 of 3.7 hours, and high maximum plasma concentrations (Cmax of 775 ng/mL)[1].

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

432.44

Formula

C21H23F3N6O
CAS 号

2499966-67-3
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]. Lexian Tong, et al. Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. J Med Chem. 2022 Feb 24;65(4):3229-3248.

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

FLT3-IN-12

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。

FLT3-IN-12 

FLT3-IN-12 是一种有效的、选择性的、具有口服活性的 FLT3 激酶抑制剂，对 FLT3-WT 和 FLT3-D835Y 的 IC50 分别为 1.48 nM 和 2.87 nM。FLT3-IN-12 具有比 c-KIT 高的选择性 (>1000 倍)。FLT3-IN-12 具有出色的抗急性髓性白血病活性 (MV4-11细胞，IC50 为 0.75 nM)。

FLT3-IN-12

FLT3-IN-12 Chemical Structure

CAS No. : 2499966-67-3

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

FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM)[1].

IC50 & Target

IC50: 1.48 nM (FLT3-WT) and 2.87 nM (FLT3-D835Y)[1]
体外研究
(In Vitro)

FLT3-IN-12 (compound 36) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y with the IC50 range is 0.16-14.5 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)

Oral administration of FLT3-IN-12 (compound 36) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting a tumor growth inhibitory rate of 95.1%. Importantly, FLT3-IN-12 could prolong the mouse survival time in the FLT3-ITD-TKD dual mutation syngeneic mouse model (BaF3-FLT3-ITD-D835Y) at a dose of 6 mg/kg p.o. bid/4W[1].
FLT3-IN-12 (compound 36; 20 mg/kg; oral administration) exhibits excellent plasma exposure (area under the curve (AUC)0–∞ of 5278 ng·h/mL), T1/2 of 3.7 hours, and high maximum plasma concentrations (Cmax of 775 ng/mL)[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

432.44

Formula

C21H23F3N6O
CAS 号

2499966-67-3
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]. Lexian Tong, et al. Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. J Med Chem. 2022 Feb 24;65(4):3229-3248.

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

FLT3/CDK4-IN-1

发表于由

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

FLT3/CDK4-IN-1 

FLT3/CDK4-IN-1 是一种有效的、高选择性且具有口服活性的 FLT3/CDK4 双重抑制剂 (FLT3 与 CDK4 的 IC50 为 7 和 11 nM)。FLT3/CDK4-IN-1 对某些癌细胞具有抗增殖活性，在体内具有良好的抗肿瘤作用。

FLT3/CDK4-IN-1

FLT3/CDK4-IN-1 Chemical Structure

CAS No. : 2762296-44-4

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

FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo[1].

IC50 & Target

CDK4

7 nM (IC50)

体外研究
(In Vitro)

FLT3/CDK4-IN-1 (compound 23k) (various concentrations; 72 hours) has better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively[1].
FLT3/CDK4-IN-1 (12.5-200 nM; 24 hours) arrests the cell cycle in G1 phase in a concentration-dependent manner[1].
FLT3/CDK4-IN-1 (200-3200 nM; 48 hours) induces apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and is more capable in MV4-11 than HCT-116[1].
FLT3/CDK4-IN-1 (0-100 nM; 2hours) inhibits the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner[1].

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

Cell Proliferation Assay

Cell Line: MV4-11, HCT-116, MDA-MB-436[1]
Concentration: Various concentrations
Incubation Time: 72 hours
Result: FLT3/CDK4-IN-1 had better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively.

Cell Cycle Analysis

Cell Line: MV4-11, HCT-116[1]
Concentration: 12.5, 25, 50, 100 and 200 nM
Incubation Time: 24 hours
Result: Arrested the cell cycle in G1 phase in a concentration-dependent manner.

Apoptosis Analysis

Cell Line: MV4-11, HCT-116[1]
Concentration: 200, 400, 800, 1600 and 3200 nM
Incubation Time: 48 hours
Result: Induced apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and was more capable in MV4-11 than HCT-116.

Western Blot Analysis

Cell Line: MV4-11[1]
Concentration: 0, 5, 10, 20, 40, 100 nM
Incubation Time: 2 hours
Result: Inhibited the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner.

体内研究
(In Vivo)

FLT3/CDK4-IN-1 (100 and 200 mg/kg; p.o.; 14 days, once daily) significantly inhibits the tumor growth at the dose of 200 mg/kg[1].

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

Animal Model: Female nu/nu mice (MV4-11-injected)[1]
Dosage: 100 and 200 mg/kg
Administration: p.o.; 14 days, once daily
Result: Significantly inhibited the tumor growth at the dose of 200 mg/kg while no significant antitumor effect at 100 mg/kg.

分子量

478.54

Formula

C25H28F2N8
CAS 号

2762296-44-4
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]. Li X, et al. Synthesis and biological evaluation of 6-(pyrimidin-4-yl)-1H-pyrazolo[4,3-b]pyridine derivatives as novel dual FLT3/CDK4 inhibitors. Bioorg Chem. 2022;121:105669.

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

FLT3/CDK4-IN-1

发表于由

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

FLT3/CDK4-IN-1 

FLT3/CDK4-IN-1 是一种有效的、高选择性且具有口服活性的 FLT3/CDK4 双重抑制剂 (FLT3 与 CDK4 的 IC50 为 7 和 11 nM)。FLT3/CDK4-IN-1 对某些癌细胞具有抗增殖活性，在体内具有良好的抗肿瘤作用。

FLT3/CDK4-IN-1

FLT3/CDK4-IN-1 Chemical Structure

CAS No. : 2762296-44-4

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

FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo[1].

IC50 & Target

CDK4

7 nM (IC50)

体外研究
(In Vitro)

FLT3/CDK4-IN-1 (compound 23k) (various concentrations; 72 hours) has better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively[1].
FLT3/CDK4-IN-1 (12.5-200 nM; 24 hours) arrests the cell cycle in G1 phase in a concentration-dependent manner[1].
FLT3/CDK4-IN-1 (200-3200 nM; 48 hours) induces apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and is more capable in MV4-11 than HCT-116[1].
FLT3/CDK4-IN-1 (0-100 nM; 2hours) inhibits the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner[1].

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

Cell Proliferation Assay

Cell Line: MV4-11, HCT-116, MDA-MB-436[1]
Concentration: Various concentrations
Incubation Time: 72 hours
Result: FLT3/CDK4-IN-1 had better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively.

Cell Cycle Analysis

Cell Line: MV4-11, HCT-116[1]
Concentration: 12.5, 25, 50, 100 and 200 nM
Incubation Time: 24 hours
Result: Arrested the cell cycle in G1 phase in a concentration-dependent manner.

Apoptosis Analysis

Cell Line: MV4-11, HCT-116[1]
Concentration: 200, 400, 800, 1600 and 3200 nM
Incubation Time: 48 hours
Result: Induced apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and was more capable in MV4-11 than HCT-116.

Western Blot Analysis

Cell Line: MV4-11[1]
Concentration: 0, 5, 10, 20, 40, 100 nM
Incubation Time: 2 hours
Result: Inhibited the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner.

体内研究
(In Vivo)

FLT3/CDK4-IN-1 (100 and 200 mg/kg; p.o.; 14 days, once daily) significantly inhibits the tumor growth at the dose of 200 mg/kg[1].

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

Animal Model: Female nu/nu mice (MV4-11-injected)[1]
Dosage: 100 and 200 mg/kg
Administration: p.o.; 14 days, once daily
Result: Significantly inhibited the tumor growth at the dose of 200 mg/kg while no significant antitumor effect at 100 mg/kg.

分子量

478.54

Formula

C25H28F2N8
CAS 号

2762296-44-4
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]. Li X, et al. Synthesis and biological evaluation of 6-(pyrimidin-4-yl)-1H-pyrazolo[4,3-b]pyridine derivatives as novel dual FLT3/CDK4 inhibitors. Bioorg Chem. 2022;121:105669.

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

FLT3/CDK4-IN-1

发表于由

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

FLT3/CDK4-IN-1 

FLT3/CDK4-IN-1 是一种有效的、高选择性且具有口服活性的 FLT3/CDK4 双重抑制剂 (FLT3 与 CDK4 的 IC50 为 7 和 11 nM)。FLT3/CDK4-IN-1 对某些癌细胞具有抗增殖活性，在体内具有良好的抗肿瘤作用。

FLT3/CDK4-IN-1

FLT3/CDK4-IN-1 Chemical Structure

CAS No. : 2762296-44-4

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

FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo[1].

IC50 & Target

CDK4

7 nM (IC50)

体外研究
(In Vitro)

FLT3/CDK4-IN-1 (compound 23k) (various concentrations; 72 hours) has better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively[1].
FLT3/CDK4-IN-1 (12.5-200 nM; 24 hours) arrests the cell cycle in G1 phase in a concentration-dependent manner[1].
FLT3/CDK4-IN-1 (200-3200 nM; 48 hours) induces apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and is more capable in MV4-11 than HCT-116[1].
FLT3/CDK4-IN-1 (0-100 nM; 2hours) inhibits the phosphorylation of FLT3 at Tyr589/591 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.

Cell Proliferation Assay

Cell Line: MV4-11, HCT-116, MDA-MB-436[1]
Concentration: Various concentrations
Incubation Time: 72 hours
Result: FLT3/CDK4-IN-1 had better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively.

Cell Cycle Analysis

Cell Line: MV4-11, HCT-116[1]
Concentration: 12.5, 25, 50, 100 and 200 nM
Incubation Time: 24 hours
Result: Arrested the cell cycle in G1 phase in a concentration-dependent manner.

Apoptosis Analysis

Cell Line: MV4-11, HCT-116[1]
Concentration: 200, 400, 800, 1600 and 3200 nM
Incubation Time: 48 hours
Result: Induced apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and was more capable in MV4-11 than HCT-116.

Western Blot Analysis

Cell Line: MV4-11[1]
Concentration: 0, 5, 10, 20, 40, 100 nM
Incubation Time: 2 hours
Result: Inhibited the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner.

体内研究
(In Vivo)

FLT3/CDK4-IN-1 (100 and 200 mg/kg; p.o.; 14 days, once daily) significantly inhibits the tumor growth at the dose of 200 mg/kg[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 nu/nu mice (MV4-11-injected)[1]
Dosage: 100 and 200 mg/kg
Administration: p.o.; 14 days, once daily
Result: Significantly inhibited the tumor growth at the dose of 200 mg/kg while no significant antitumor effect at 100 mg/kg.

分子量

478.54

Formula

C25H28F2N8
CAS 号

2762296-44-4
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]. Li X, et al. Synthesis and biological evaluation of 6-(pyrimidin-4-yl)-1H-pyrazolo[4,3-b]pyridine derivatives as novel dual FLT3/CDK4 inhibitors. Bioorg Chem. 2022;121:105669.

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

FLT3-IN-11

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。

FLT3-IN-11 

FLT3-IN-11 (compound 30) 是一种有效、选择性和具有口服活性的 FLT3 激酶抑制剂，对野生型 FLT3 和 FLT3-D835Y 的 IC50 分别为 7.22 nM 和 4.95 nM。FLT3-IN-11 对 FLT3 的选择性高于 c-KIT (>1000 倍)。FLT3-IN-11 具有出色的抗急性髓性白血病 (AML) 活性 (MV4-11 细胞，IC50 为 3.2 nM)。

FLT3-IN-11

FLT3-IN-11 Chemical Structure

CAS No. : 2499966-50-4

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

FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM)[1].

IC50 & Target

IC50: 7.22 nM (wild-type FLT3) and 4.95 nM (FLT3-D835Y)[1]
体外研究
(In Vitro)

FLT3-IN-11 (compound 30) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y[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)

Oral administration of FLT3-IN-11 (compound 30) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting tumor growth inhibitory rates of 83.5%[1].

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

422.45

Formula

C20H25F3N6O
CAS 号

2499966-50-4
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]. Lexian Tong, et al. Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. J Med Chem. 2022 Feb 24;65(4):3229-3248.

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

FLT3-IN-11

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。

FLT3-IN-11 

FLT3-IN-11 (compound 30) 是一种有效、选择性和具有口服活性的 FLT3 激酶抑制剂，对野生型 FLT3 和 FLT3-D835Y 的 IC50 分别为 7.22 nM 和 4.95 nM。FLT3-IN-11 对 FLT3 的选择性高于 c-KIT (>1000 倍)。FLT3-IN-11 具有出色的抗急性髓性白血病 (AML) 活性 (MV4-11 细胞，IC50 为 3.2 nM)。

FLT3-IN-11

FLT3-IN-11 Chemical Structure

CAS No. : 2499966-50-4

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

FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM)[1].

IC50 & Target

IC50: 7.22 nM (wild-type FLT3) and 4.95 nM (FLT3-D835Y)[1]
体外研究
(In Vitro)

FLT3-IN-11 (compound 30) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y[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)

Oral administration of FLT3-IN-11 (compound 30) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting tumor growth inhibitory rates of 83.5%[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

422.45

Formula

C20H25F3N6O
CAS 号

2499966-50-4
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]. Lexian Tong, et al. Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. J Med Chem. 2022 Feb 24;65(4):3229-3248.

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

FLT3-IN-11

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。

FLT3-IN-11 

FLT3-IN-11 (compound 30) 是一种有效、选择性和具有口服活性的 FLT3 激酶抑制剂，对野生型 FLT3 和 FLT3-D835Y 的 IC50 分别为 7.22 nM 和 4.95 nM。FLT3-IN-11 对 FLT3 的选择性高于 c-KIT (>1000 倍)。FLT3-IN-11 具有出色的抗急性髓性白血病 (AML) 活性 (MV4-11 细胞，IC50 为 3.2 nM)。

FLT3-IN-11

FLT3-IN-11 Chemical Structure

CAS No. : 2499966-50-4

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

FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM)[1].

IC50 & Target

IC50: 7.22 nM (wild-type FLT3) and 4.95 nM (FLT3-D835Y)[1]
体外研究
(In Vitro)

FLT3-IN-11 (compound 30) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y[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)

Oral administration of FLT3-IN-11 (compound 30) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting tumor growth inhibitory rates of 83.5%[1].

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

422.45

Formula

C20H25F3N6O
CAS 号

2499966-50-4
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]. Lexian Tong, et al. Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. J Med Chem. 2022 Feb 24;65(4):3229-3248.

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

FLT3-IN-14

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。

FLT3-IN-14 

FLT3-IN-14 是一种有效的 FLT3 抑制剂，对 FLT3-WT 和 FLT3-ITD 的 IC50 分别为 5.6 nM 和 1.4 nM。FLT3-IN-14 降低 FLT3 (Y591) 磷酸化，将细胞周期阻滞在 G1 期，诱导细胞凋亡 (apoptosis)。

FLT3-IN-14

FLT3-IN-14 Chemical Structure

CAS No. : 2620551-45-1

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

FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model[1].

IC50 & Target

IC50: 1.4 nM (FLT-ITD), 5.6 nM (FLT3-WT)[1]
体外研究
(In Vitro)

FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC50s of 0.011-1.582 μM[1].
FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI50 greater than 10 μM, in resting lymphocytes[1].
FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner[1].
FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines[1].
FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3[1].

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

Cell Proliferation Assay

Cell Line: MOLT-4 , HL-60, KG-1, KG-1a, MOLM-13, MV4-11, NOMO-1, OCI-AML2, PL-21, THP-1, K-562, KCL-22[1]
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of these twelve haematological cell lines with IC50s of 0.011-1.582 μM.

Cell Cytotoxicity Assay

Cell Line: PBL[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Exhibited low toxicity, with GI50 greater than 10 μM, in resting lymphocytes.

Apoptosis Analysis

Cell Line: MV4-11[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 and 48 hours
Result: Accumulated annexin-V positive cells in a concentration and time-dependent manner.

Cell Cycle Analysis

Cell Line: MOLM-13 and MV-14[1]
Concentration: 25, 50, 75 and 100 nM
Incubation Time: 24 and 48 hours
Result: Induced a significant G1 arrest in both cell lines.

Western Blot Analysis

Cell Line: MV-14[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 hours
Result: Induced the dephosphorylation of FLT3.

体内研究
(In Vivo)

FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity[1].

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

Animal Model: NOD/SCID female mice (subcutaneously implanted MV4-11)[1]
Dosage: 1.0 and 3.0 mg/kg
Administration: IP; daily for 28 days
Result: Significantly reduced tumor growth by 44.1% and 55.2% at 1 and 3 mg/kg, respectively.

分子量

472.56

Formula

C25H24N6O2S
CAS 号

2620551-45-1
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]. Cilibrasi V, Spanò V, Bortolozzi R, et al. Synthesis of 2H-Imidazo[2′,1′:2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. Eur J Med Chem. 2022;235:114292.

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

FLT3-IN-14

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。

FLT3-IN-14 

FLT3-IN-14 是一种有效的 FLT3 抑制剂，对 FLT3-WT 和 FLT3-ITD 的 IC50 分别为 5.6 nM 和 1.4 nM。FLT3-IN-14 降低 FLT3 (Y591) 磷酸化，将细胞周期阻滞在 G1 期，诱导细胞凋亡 (apoptosis)。

FLT3-IN-14

FLT3-IN-14 Chemical Structure

CAS No. : 2620551-45-1

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

FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model[1].

IC50 & Target

IC50: 1.4 nM (FLT-ITD), 5.6 nM (FLT3-WT)[1]
体外研究
(In Vitro)

FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC50s of 0.011-1.582 μM[1].
FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI50 greater than 10 μM, in resting lymphocytes[1].
FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner[1].
FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines[1].
FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3[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 Proliferation Assay

Cell Line: MOLT-4 , HL-60, KG-1, KG-1a, MOLM-13, MV4-11, NOMO-1, OCI-AML2, PL-21, THP-1, K-562, KCL-22[1]
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of these twelve haematological cell lines with IC50s of 0.011-1.582 μM.

Cell Cytotoxicity Assay

Cell Line: PBL[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Exhibited low toxicity, with GI50 greater than 10 μM, in resting lymphocytes.

Apoptosis Analysis

Cell Line: MV4-11[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 and 48 hours
Result: Accumulated annexin-V positive cells in a concentration and time-dependent manner.

Cell Cycle Analysis

Cell Line: MOLM-13 and MV-14[1]
Concentration: 25, 50, 75 and 100 nM
Incubation Time: 24 and 48 hours
Result: Induced a significant G1 arrest in both cell lines.

Western Blot Analysis

Cell Line: MV-14[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 hours
Result: Induced the dephosphorylation of FLT3.

体内研究
(In Vivo)

FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity[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: NOD/SCID female mice (subcutaneously implanted MV4-11)[1]
Dosage: 1.0 and 3.0 mg/kg
Administration: IP; daily for 28 days
Result: Significantly reduced tumor growth by 44.1% and 55.2% at 1 and 3 mg/kg, respectively.

分子量

472.56

Formula

C25H24N6O2S
CAS 号

2620551-45-1
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]. Cilibrasi V, Spanò V, Bortolozzi R, et al. Synthesis of 2H-Imidazo[2′,1′:2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. Eur J Med Chem. 2022;235:114292.

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

FLT3-IN-14

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。

FLT3-IN-14 

FLT3-IN-14 是一种有效的 FLT3 抑制剂，对 FLT3-WT 和 FLT3-ITD 的 IC50 分别为 5.6 nM 和 1.4 nM。FLT3-IN-14 降低 FLT3 (Y591) 磷酸化，将细胞周期阻滞在 G1 期，诱导细胞凋亡 (apoptosis)。

FLT3-IN-14

FLT3-IN-14 Chemical Structure

CAS No. : 2620551-45-1

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

FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model[1].

IC50 & Target

IC50: 1.4 nM (FLT-ITD), 5.6 nM (FLT3-WT)[1]
体外研究
(In Vitro)

FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC50s of 0.011-1.582 μM[1].
FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI50 greater than 10 μM, in resting lymphocytes[1].
FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner[1].
FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines[1].
FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3[1].

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

Cell Proliferation Assay

Cell Line: MOLT-4 , HL-60, KG-1, KG-1a, MOLM-13, MV4-11, NOMO-1, OCI-AML2, PL-21, THP-1, K-562, KCL-22[1]
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of these twelve haematological cell lines with IC50s of 0.011-1.582 μM.

Cell Cytotoxicity Assay

Cell Line: PBL[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Exhibited low toxicity, with GI50 greater than 10 μM, in resting lymphocytes.

Apoptosis Analysis

Cell Line: MV4-11[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 and 48 hours
Result: Accumulated annexin-V positive cells in a concentration and time-dependent manner.

Cell Cycle Analysis

Cell Line: MOLM-13 and MV-14[1]
Concentration: 25, 50, 75 and 100 nM
Incubation Time: 24 and 48 hours
Result: Induced a significant G1 arrest in both cell lines.

Western Blot Analysis

Cell Line: MV-14[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 hours
Result: Induced the dephosphorylation of FLT3.

体内研究
(In Vivo)

FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity[1].

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

Animal Model: NOD/SCID female mice (subcutaneously implanted MV4-11)[1]
Dosage: 1.0 and 3.0 mg/kg
Administration: IP; daily for 28 days
Result: Significantly reduced tumor growth by 44.1% and 55.2% at 1 and 3 mg/kg, respectively.

分子量

472.56

Formula

C25H24N6O2S
CAS 号

2620551-45-1
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]. Cilibrasi V, Spanò V, Bortolozzi R, et al. Synthesis of 2H-Imidazo[2′,1′:2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. Eur J Med Chem. 2022;235:114292.

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

c-Met/MEK1/Flt-3-IN-1

发表于由

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

c-Met/MEK1/Flt-3-IN-1 

Antiproliferative against-3 (comp 33) 具有良好的抗癌细胞增殖活性，对 Hela、A549 和 MCF-7 的细胞的IC50 值分别为 0.21 µM、0.39 µM 和 0.33 µM。Antiproliferative against-3 (comp 33) 剂量依赖性的诱导A549 细胞的凋亡，并将细胞阻滞在 G1 期。

c-Met/MEK1/Flt-3-IN-1

c-Met/MEK1/Flt-3-IN-1 Chemical Structure

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

Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase[1].

分子量

688.75

Formula

C39H37FN6O5
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]. Pengqin Chen, et al. Design, synthesis and anticancer evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 1,8-naphthyridine-3-carboxamide moiety as novel multi-target TKIs. Bioorg Chem. 2022 Apr;121:105672.

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

c-Met/MEK1/Flt-3-IN-1

发表于由

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

c-Met/MEK1/Flt-3-IN-1 

Antiproliferative against-3 (comp 33) 具有良好的抗癌细胞增殖活性，对 Hela、A549 和 MCF-7 的细胞的IC50 值分别为 0.21 µM、0.39 µM 和 0.33 µM。Antiproliferative against-3 (comp 33) 剂量依赖性的诱导A549 细胞的凋亡，并将细胞阻滞在 G1 期。

c-Met/MEK1/Flt-3-IN-1

c-Met/MEK1/Flt-3-IN-1 Chemical Structure

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

Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase[1].

分子量

688.75

Formula

C39H37FN6O5
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]. Pengqin Chen, et al. Design, synthesis and anticancer evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 1,8-naphthyridine-3-carboxamide moiety as novel multi-target TKIs. Bioorg Chem. 2022 Apr;121:105672.

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

c-Met/MEK1/Flt-3-IN-1

发表于由

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c-Met/MEK1/Flt-3-IN-1 

Antiproliferative against-3 (comp 33) 具有良好的抗癌细胞增殖活性，对 Hela、A549 和 MCF-7 的细胞的IC50 值分别为 0.21 µM、0.39 µM 和 0.33 µM。Antiproliferative against-3 (comp 33) 剂量依赖性的诱导A549 细胞的凋亡，并将细胞阻滞在 G1 期。

c-Met/MEK1/Flt-3-IN-1

c-Met/MEK1/Flt-3-IN-1 Chemical Structure

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生物活性

Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase[1].

分子量

688.75

Formula

C39H37FN6O5
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]. Pengqin Chen, et al. Design, synthesis and anticancer evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 1,8-naphthyridine-3-carboxamide moiety as novel multi-target TKIs. Bioorg Chem. 2022 Apr;121:105672.

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FLT3/D835Y-IN-1

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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。

FLT3/D835Y-IN-1 

FLT3/D835Y-IN-1 (化合物13a) 是一种口服有效且选择性的 FLT3 和FLT3/D835Y 抑制剂，其 IC50 值分别为 0.26 nM 和 0.18 nM。FLT3/D835Y-IN-1 还能阻断肿瘤生长，具有抗癌作用，可以用于研究急性髓系白血病。

FLT3/D835Y-IN-1

FLT3/D835Y-IN-1 Chemical Structure

CAS No. : 2648799-49-7

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生物活性

FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia)[1].

IC50 & TargetFLT3/D835Y

FLT3/D835Y

0.18 nM (IC50)

体外研究
(In Vitro)

FLT3/D835Y-IN-1 (compound 13a) (100 nM, 3 h) potently inhibits Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L cell lines, and AML cells proliferation[1].
FLT3/D835Y-IN-1 (3-30 nM, 16 h) significantly inhibit FLT3, AKT, ERK, and STAT5 pathways[1].

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

Cell Proliferation Assay

Cell Line: Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, and Ba/F3-FLT3-ITD-F691L cell lines, AML cells[1]
Concentration: 100 nM
Incubation Time: 3 h
Result: Inhibited Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L, MV4-11, MOLM14, and MOLM14-ITD/D835Y proliferation, with GI50 values of 0.59, 0.73, 5.54, 1.30, 6.20, and 4.58 nM, respectively.

Western Blot Analysis

Cell Line: MOLM14-ITD/D835Y and MOLM14-ITD/F691L cells[1].
Concentration: 3, 10, and 30 nM
Incubation Time: 16 h
Result: Significantly inhibited the FLT3, AKT, ERK, and STAT5 pathways at lower dosages.

体内研究
(In Vivo)

FLT3/D835Y-IN-1 (10 mg/kg, IP, daily, 6 days per week) significantly suppresses tumor growth and exhibits potent antitumor activity against MOLM14-ITD/D835Y cells[1].
FLT3/D835Y-IN-1 (10 mg/kg, IV or Orally, single) displays extremely low AUC and high clearance[1].
Pharmacokinetic Parameters of FLT3/D835Y-IN-1 in ICR mice[1].

Parameters 13a
AUClast (ng*h/mL) 1360 ± 110
CL (L/h/kg) 6.96 ± 0.66
Vss (L/kg) 14.8 ± 0.7
T1/2 (h) 1.5 ± 0.1

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

Animal Model: NOD/SCID mice (6 weeks, male, nine mice per group)[1]
Dosage: 10 mg/kg
Administration: IP, daily, 6 days per week, from day 7 to day 29
Result: Significantly suppressed tumor growth.
Animal Model: ICR mice (7–8 weeks, male)[1]
Dosage: 10 mg/kg, dissolved in a solution (10% DMSO, 40% PEG400, and 50% PBS)
Administration: IV or Orally, single (Pharmacokinetic Analysis)
Result: Displayed extremely low AUC and high clearance.

分子量

403.43

Formula

C22H21N5O3
CAS 号

2648799-49-7
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]. Lee JH, Shin JE, Kim W, et al. Discovery of indirubin-3′-aminooxy-acetamide derivatives as potent and selective FLT3/D835Y mutant kinase inhibitors for acute myeloid leukemia. Eur J Med Chem. 2022 Apr 21;237:114356.

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FLT3-IN-15

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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。

FLT3-IN-15 

FLT3-IN-15 是一种有效且具有口服活性的 FLT3 抑制剂，对 FLT3 和 FLT3/D835Y 的 IC50 分别为 0.87 nM 和 0.32 nM。FLT3-IN-15 可用于研究急性髓系白血病。

FLT3-IN-15

FLT3-IN-15 Chemical Structure

CAS No. : 2435562-99-3

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生物活性

FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia[1].

IC50 & Target

IC50: 0.87 nM (FLT3), 0.32 nM (FLT3/D835Y)[1]
体外研究
(In Vitro)

FLT3-IN-15 (compound 36) (0-100 nM) exhibits anti-proliferative activities against MOLM14 cell lines[1].
FLT3-IN-15 (0-1 μM; 72 hours) shows extremely more sensitive against MV4-11 cells than K562 cell line, and displayed good safety profiles against other cancer cell lines[1].
FLT3-IN-15 (0.01-1 μM; 4 hours) shows strongly blockage of the phosphorylation of STAT5 and Erk1/2 in MV4-11 cells[1].

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

Cell Proliferation Assay

Cell Line: MOLM14 wild type cells, MOLM14-ITD cells, MOLM14-ITD-D835Y cells, MOLM14-ITD-F691L cells[1]
Concentration: 0-100 nM
Incubation Time:
Result: Exhibited anti-proliferative activities against MOLM14 cell lines, with GI50s of 4.88 ± 0.67 nM, 1.85 ± 0.06 nM, 1.87 ± 0.36 nM and 3.27 ± 0.99 nM in MOLM14 wild type cells, MOLM14-ITD cells, MOLM14-ITD-D835Y cells and MOLM14-ITD-F691L cells, respectively.

Cell Proliferation Assay

Cell Line: MV4-11, K562, A549, HepG2, MDA-MB-231, HCT-116, PC3 and SK-OV-3[1]
Concentration: 0-1 μM
Incubation Time: 72 hours
Result: Showed extremely more sensitive against MV4-11 cells (GI50 = 1 nM) than K562 cell line, and displayed good safety profiles against other cancer cell lines.

Western Blot Analysis

Cell Line: MV4-11[1]
Concentration: 10 nM, 100 nM and 1 μM
Incubation Time: 4 hours
Result: Showed strongly blockage of the phosphorylation of STAT5 and Erk1/2.

体内研究
(In Vivo)

FLT3-IN-15 (20 mg/kg; PO; daily, for 21 days) results in the rapid and complete remission of tumors in all mice[1].
FLT3-IN-15 (2000 mg/kg; PO; single) causes one female mouse died at day 6, and the LD50 value is calculated as 4,950 mg/kg in female mice[1].
FLT3-IN-15 (10 μM) shows 21.4% inhibition of hERG ligand binding[1].
FLT3-IN-15 (10 mg/kg; PO and IV; single) exhibits an AUClast of 25.0 μg·min/mL, a Cmax of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%[1].
Pharmacokinetic Parameters of FLT3-IN-15 in male ICR mice[1].

PO (10 mg/kg) IV (10 mg/kg)
AUClast (μg·min/mL) 25.0 ± 11.6 58.5 ± 57.4
AUCinf (μg·min/mL) 62.1 ± 58.6 103.4 ± 95.3
MRT (hr) 2811.3 ± 2713.0 1257.1 ± 1084.1
T1/2 (hr) 1775.7 ± 1901.0 1099.2 ± 945.8
CL (mL/min/kg) 158.7 ± 98.7
VSS (L/kg) 127891 ± 104764
Cmax (ng/mL) 36.5 ± 24.3
Tmax (min) 390.0 ± 366.0
Xu, 24h (%) 0.001 ± 0.0 0.002 ± 0.002
GI24h (%) 0.05 ± 0.05 0.24 ± 0.02
F (%) 42.9

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

Animal Model: BALB/c nu/nu (injected with MV4-11)[1]
Dosage: 20 mg/kg
Administration: PO; daily, for 21 days
Result: Resulted in the rapid and complete remission of tumors in all mice, and no weight loss or any other signs of toxicity during the administration period.
Animal Model: Female ICR mice[1]
Dosage: 2000 mg/kg
Administration: PO; single
Result: Caused one female mouse of the 2,000 mg/kg group died at day 6 and the approximate lethal dose (ALD) is determined over 2,000 mg/kg in male mice and 2,000 mg/kg in female mice, respectively; the LD50 value was calculated as 4,950 mg/kg in female mice.
Animal Model: Male ICR mice[1]
Dosage: 10 mg/kg
Administration: PO and IV; single (Pharmacokinetics Analysis)
Result: Exhibited an AUClast of 25.0 μg·min/mL, a Cmax of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%.

分子量

443.90

Formula

C22H23ClFN5O2
CAS 号

2435562-99-3
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]. Jeong P, Moon Y, Lee JH, et al. Discovery of orally active indirubin-3′-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia. Eur J Med Chem. 2020;195:112205.

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BSc5371

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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。

BSc5371 

BSc5371 是一种有效的、不可逆的 FLT3 抑制剂，对 FLT3 突变体 FLT3(D835H)，FLT3(ITD, D835V)，FLT3(ITD, F691L)，FLT3-ITD 和野生型 FLT3wt 的 Kd 值分别为 1.3，0.83，1.5，5.8 和 2.3 nM。BSc5371 对 FLT3 依赖性的细胞具有细胞毒性。

BSc5371

BSc5371 Chemical Structure

CAS No. : 2286419-03-0

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生物活性

BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines[1].

IC50 & Target

Kd: 1.3 nM (LT3(D835H)), 0.83 nM (LT3(ITD, D835V)), 1.5 nM (LT3(ITD, F691L)), 5.8 nM (FLT3-ITD), 2.3 nM (FLT3wt)[1]
体外研究
(In Vitro)

BSc5371 (5 μM-0.5 nM, 77 hours) exhibits inhibitory activity against FLT3-mutated (MV4-11) cells, with an IC50 of 6 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.

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 0.5 nM, 2.5 nM, 5 nM, 25 nM, 50 nM, 250 nM, 500 nM and 5 μM
Incubation Time: 77 hours
Result: Exhibited inhibitory activity against MV4-11 cells, with an IC50 of 6 nM.

分子量

485.60

Formula

C24H31N5O4S
CAS 号

2286419-03-0
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]. Bensinger D, et al. Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. J Med Chem. 2019 Mar 14;62(5):2428-2446.

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FLT3-IN-4

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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。

FLT3-IN-4 

FLT3-IN-4 是一种口服有效的 Fms 样酪氨酸受体激酶 3 (FLT3; IC50= 7 nM) 抑制剂，可用于急性髓性白血病的研究。

FLT3-IN-4

FLT3-IN-4 Chemical Structure

CAS No. : 2304799-09-3

规格 价格 是否有货
5 mg ￥4800 询问价格 & 货期
10 mg ￥8000 询问价格 & 货期
25 mg ￥15500 询问价格 & 货期

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生物活性

FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia[1].

体外研究
(In Vitro)

FLT3-IN-4 (Compound 9u) shows potent inhibitory activities against MV4-11 and Molm-13 cells with IC50 values are 0.089±0.001 nM and 0.022±0.003 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.
分子量

431.49

Formula

C23H25N7O2
CAS 号

2304799-09-3
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]. Yuan X, et al. Identification of Pyrrolo[2,3- d]pyrimidine-Based Derivatives as Potent and Orally Effective Fms-like Tyrosine Receptor Kinase 3 (FLT3) Inhibitors for Treating Acute Myelogenous Leukemia. J Med Chem. 2019 Apr 25;62(8):4158-4173.

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Quizartinib(Synonyms: 奎扎替尼; AC220)

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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。

Quizartinib (Synonyms: 奎扎替尼; AC220) 纯度: 98.87%

Quizartinib (AC220) 是一种具有口服活性的、高选择性的，有效的第二代 Ⅱ 型 FLT3 (type II FLT3) 酪氨酸激酶抑制剂，Kd 值为 1.6 nM。Quizartinib 抑制 Wt FLT3 和 突变型 FLT3-ITD 自磷酸化，IC50 分别为 4.1 nM 和 1.1 nM。Quizartinib 可以通过优化的 linker 与 VHL 配体连接，从而形成 PROTAC Flt3 降解剂。Quizartinib 诱导细胞凋亡 (apoptosis)。

Quizartinib(Synonyms: 奎扎替尼; AC220)

Quizartinib Chemical Structure

CAS No. : 950769-58-1

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50 mg ￥4200 In-stock
100 mg ￥7200 In-stock
200 mg ￥9950 In-stock
500 mg ￥19500 In-stock
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生物活性

Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis[1].

IC50 & Target

Kd: 1.6±0.7 nM (Flt3)[1]
体外研究
(In Vitro)

Quizartinib (AC220) is a novel compound expressly optimized as a FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). Quizartinib inhibits FLT3-WT and FLT3-ITD autophosphorylation with IC50 of 4.2±0.3 nM and 1.1±0.1 nM, respectively. Quizartinib inhibits MV4-11 and A375 cells with IC50 of 0.56±0.3 nM and >10 000 nM, respectively. Quizartinib inhibits FLT3 with low nanomolar potency in cellular assays and is highly selective when screened against the majority of the human protein kinome[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)

Quizartinib (AC220) inhibits FLT3 activity in vivo, significantly extends survival in a mouse model of FLT3-ITD AML at doses as low as 1 mg/kg when dosed orally once a day, eradicates tumors in a FLT3-dependent mouse xenograft model at 10 mg/kg, and potently inhibits FLT3 activity in primary patient cells. The oral bioavailability of Quizartinib, determined in rats by comparing oral and intravenous pharmacokinetics at 3 mg/kg, is approximately 40%. A single 10 mg/kg dose of Quizartinib is administered by oral gavage, and mice are killed at 2 time points after dosing, using groups of 4 animals each. Quantitation of total FLT3 and phospho-FLT3 in tumor samples revealed time-dependent inhibition of FLT3 autophosphorylation. FLT3 activity is inhibited by 90% at 2 hours, and 40% at 24 hours after administration. The extent of inhibition therefore correlated well with the expected free Quizartinib plasma levels, based on pharmacokinetic experiments[1].

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

分子量

560.67

Formula

C29H32N6O4S
CAS 号

950769-58-1
中文名称

奎扎替尼
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 : ≥ 33 mg/mL (58.86 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 1.7836 mL 8.9179 mL 17.8358 mL
5 mM 0.3567 mL 1.7836 mL 3.5672 mL
10 mM 0.1784 mL 0.8918 mL 1.7836 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:
  • 1.

    Quizartinib (AC220) is prepared in vehicle (22% hydroxypropyl-β-cyclodextrin in sterile water)[2].
参考文献

  • [1]. Zarrinkar PP, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood, 2009, 114(14), 2984-2992.

    [2]. Puissant A, et al. SYK is a critical regulator of FLT3 in acute myeloid leukemia. Cancer Cell. 2014 Feb 10;25(2):226-42.

    [3]. Sun X, et al. PROTACs: great opportunities for academia and industry. Signal Transduct Target Ther. 2019 Dec 24;4:64.
Kinase Assay
[1]

KinomeScan kinase binding assays are performed. For the FLT3 assay, a kinase construct that spanned the catalytic domain only (amino acids 592 to 969) is used. This construct does not include the juxtamembrane domain and is designed to measure the intrinsic binding affinity of the open FLT3 active site for inhibitors[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 Assay
[1]

MV4-11 and RS4;11 cells are cultured in Iscove media with 10% fetal bovine serum (FBS) and RPMI complete with 10% FBS, respectively. For proliferation assays, cells are cultured overnight in low serum media (0.5% FBS), then seeded in a 96-well plate at 40 000 cells per well. Inhibitors (e.g., Quizartinib) are added to the cells and incubated at 37°C for 72 hours. Cell viability is measured using the Cell Titer-Blue Cell Viability Assay. To measure inhibition of FLT3 autophosphorylation, cells are cultured in low serum media (0.5% FBS) overnight and seeded at a density of 400 000 cells per well in a 96-well plate the following day. The cells are incubated with inhibitors (e.g., Quizartinib) for 2 hours at 37°C. To induce FLT3 autophosphorylation in RS4;11 cells, 100 ng/mL FLT3 ligand is added for 15 minutes after the 2-hour compound incubation. Cell lysates are prepared and incubated in 96-well plates precoated with a total FLT3 capture antibody. The coated plates are incubated with either a biotinylated antibody against FLT3 to detect total FLT3 or an antibody against phosphotyrosines to detect FLT3 autophosphorylation. In both cases, a SULFO-tagged streptavidin secondary antibody is used for electrochemiluminescence detection on the Meso Scale Discovery platform[1].

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

Mice[1]
Female NU/NU or severe combined immunodeficient mice are used. Quizartinib (hydrochloride salt) is formulated in 22% hydroxypropyl-β-cyclodextrin, CEP-701 is formulated in 20% gelucire 44/14 in water (vol/vol), MLN-518 and SU 11248 are formulated in 10 mM sodium citrate (pH 3.5), PKC-412 is formulated in 3:1 gelucire 44/14-propylene glycol (vol/vol), and Bay 43-9006 is formulated in 80% PEG-400. Compound concentrations are chosen to deliver the desired dose in a volume of 10 mL/kg. Compounds are administered by oral gavage and plasma samples collected 0.25, 0.5, 1, 2, 4, 6, and 24 hours after dosing. To collect plasma samples, eye bleeds (150 μL) are taken semilongitudinally using 3 groups of 3 animals each, taking 2 to 3 time points per animal to obtain a total of 3 independent plasma concentration time courses. Plasma samples and controls (25 μL) are extracted with 4 volumes of acetonitrile containing an internal standard and analyzed by liquid chromatography tandem mass spectrometry.

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

  • [1]. Zarrinkar PP, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood, 2009, 114(14), 2984-2992.

    [2]. Puissant A, et al. SYK is a critical regulator of FLT3 in acute myeloid leukemia. Cancer Cell. 2014 Feb 10;25(2):226-42.

    [3]. Sun X, et al. PROTACs: great opportunities for academia and industry. Signal Transduct Target Ther. 2019 Dec 24;4:64.

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