GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases[1].
IC50 & Target
cdk5[1] cdk2[1] GSK-3[1]
体外研究 (In Vitro)
GSK-3/CDK5/CDK2-IN-1 inhibits the phosphorylation of cdk5 peptide substrate phosphorylation, with an IC50 of less than about 50 μM[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
362.42
Formula
C21H22N4O2
CAS 号
395074-72-3
运输条件
Room temperature in continental US; may vary elsewhere.
CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.
IC50 & Target[1]
CDK8
3 nM (IC50)
体内研究 (In Vivo)
CDK8-IN-1 displays low systemic clearance, very good exposure and oral bioavailability. The tmax is 0.25 h by PO. The mean values of Cmax are 9940 μg/L, 12740 μg/L by IV and PO respectively. The values of AUC are 9378, 25952 by IV and PO 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
255.20
Formula
C11H8F3N3O
CAS 号
1629633-48-2
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
参考文献
[1]. Han X, et al. Discovery of potent and selective CDK8 inhibitors through FBDD approach. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4488-4492.
Animal Administration [1]
Mice[1] CDK8-IN-1 is administrated to mice with 5 mg/kg, 25mg/mg by IV and PO 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.
参考文献
[1]. Han X, et al. Discovery of potent and selective CDK8 inhibitors through FBDD approach. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4488-4492.
Cdk1/2 Inhibitor III 是一种选择性的 Cdk1/2 抑制剂，对 CDK1/cyclin B 作用的 IC50 值为 2.1 μM。
Cdk1/2 Inhibitor III Chemical Structure
CAS No. : 443798-55-8
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
Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor, with an IC50 of 2.1 μM for CDK1/cyclin B[1].
IC50 & Target
Cdk1/cyclin B
2.1 μM (IC50)
体外研究 (In Vitro)
Cdk1/2 Inhibitor III has weak CDK1 and cellular antiproliferative potencies[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
425.44
Formula
C15H13F2N7O2S2
CAS 号
443798-55-8
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]. Lin R, et al. Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11.
Cdk1/2 Inhibitor III 是一种选择性的 Cdk1/2 抑制剂，对 CDK1/cyclin B 作用的 IC50 值为 2.1 μM。
Cdk1/2 Inhibitor III Chemical Structure
CAS No. : 443798-55-8
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
Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor, with an IC50 of 2.1 μM for CDK1/cyclin B[1].
IC50 & Target
Cdk1/cyclin B
2.1 μM (IC50)
体外研究 (In Vitro)
Cdk1/2 Inhibitor III has weak CDK1 and cellular antiproliferative potencies[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
425.44
Formula
C15H13F2N7O2S2
CAS 号
443798-55-8
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]. Lin R, et al. Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11.
Cdk1/2 Inhibitor III 是一种选择性的 Cdk1/2 抑制剂，对 CDK1/cyclin B 作用的 IC50 值为 2.1 μM。
Cdk1/2 Inhibitor III Chemical Structure
CAS No. : 443798-55-8
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
Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor, with an IC50 of 2.1 μM for CDK1/cyclin B[1].
IC50 & Target
Cdk1/cyclin B
2.1 μM (IC50)
体外研究 (In Vitro)
Cdk1/2 Inhibitor III has weak CDK1 and cellular antiproliferative potencies[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
425.44
Formula
C15H13F2N7O2S2
CAS 号
443798-55-8
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]. Lin R, et al. Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11.
NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2[1].
IC50 & Target[1]
CDK4/D1
0.2 μM (IC50)
体外研究 (In Vitro)
NSC 625987 (10 nM, 50 nM, 100 nM) treatment attenuates the enhanced proliferation of vascular smooth muscle cells (VSMC) from spontaneously hypertensive rats (SHR) rats by about 35%[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
271.33
Formula
C15H13NO2S
CAS 号
141992-47-4
运输条件
Room temperature in continental US; may vary elsewhere.
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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
[1]. A Kubo, et al. The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4. Clin Cancer Res. 1999 Dec;5(12):4279-86.
[2]. Jasmine El Andalousi, et al.Natriuretic peptide receptor-C agonist attenuates the expression of cell cycle proteins and proliferation of vascular smooth muscle cells from spontaneously hypertensive rats: role of Gi proteins and MAPkinase/PI3kinase signaling. PLoS One. 2013 Oct 14;8(10):e76183.
NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2[1].
IC50 & Target[1]
CDK4/D1
0.2 μM (IC50)
体外研究 (In Vitro)
NSC 625987 (10 nM, 50 nM, 100 nM) treatment attenuates the enhanced proliferation of vascular smooth muscle cells (VSMC) from spontaneously hypertensive rats (SHR) rats by about 35%[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.
分子量
271.33
Formula
C15H13NO2S
CAS 号
141992-47-4
运输条件
Room temperature in continental US; may vary elsewhere.
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]. A Kubo, et al. The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4. Clin Cancer Res. 1999 Dec;5(12):4279-86.
[2]. Jasmine El Andalousi, et al.Natriuretic peptide receptor-C agonist attenuates the expression of cell cycle proteins and proliferation of vascular smooth muscle cells from spontaneously hypertensive rats: role of Gi proteins and MAPkinase/PI3kinase signaling. PLoS One. 2013 Oct 14;8(10):e76183.
NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2[1].
IC50 & Target[1]
CDK4/D1
0.2 μM (IC50)
体外研究 (In Vitro)
NSC 625987 (10 nM, 50 nM, 100 nM) treatment attenuates the enhanced proliferation of vascular smooth muscle cells (VSMC) from spontaneously hypertensive rats (SHR) rats by about 35%[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
271.33
Formula
C15H13NO2S
CAS 号
141992-47-4
运输条件
Room temperature in continental US; may vary elsewhere.
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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
[1]. A Kubo, et al. The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4. Clin Cancer Res. 1999 Dec;5(12):4279-86.
[2]. Jasmine El Andalousi, et al.Natriuretic peptide receptor-C agonist attenuates the expression of cell cycle proteins and proliferation of vascular smooth muscle cells from spontaneously hypertensive rats: role of Gi proteins and MAPkinase/PI3kinase signaling. PLoS One. 2013 Oct 14;8(10):e76183.
CDK12-IN-4 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 0.641 μM。CDK12-IN-4 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50>20 μM) 和 CDK9/Cyclin T1 (IC50>20 μM) 没有影响(WO2021116178A1)。
CDK12-IN-4 Chemical Structure
CAS No. : 2651196-69-7
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
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1)[1].
IC50 & Target[1]
CDK12
0.641 μM (IC50)
CDK2/cyclinE
>20 μM (IC50)
CDK9/cyclinT1
>20 μM (IC50)
体外研究 (In Vitro)
CDK12-IN-4 (Example 172) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.626 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-4 has antproliferative activity in MDA-MB-231 cells (IC50=0.535 nM) and CAL-120 cells (IC50=2.43 nM)[1]. CDK12-IN-4 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 581[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
426.42
Formula
C20H20F2N8O
CAS 号
2651196-69-7
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.
CDK12-IN-6 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 1.19 μM。CDK12-IN-6 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50>20 μM) 和 CDK9/Cyclin T1 (IC50>20 μM) 没有影响(WO2021116178A1)。
CDK12-IN-6 Chemical Structure
CAS No. : 2651196-71-1
规格
是否有货
5 mg
询价
10 mg
询价
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
生物活性
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1)[1].
IC50 & Target[1]
CDK12
1.19 μM (IC50)
CDK2/cyclinE
>20 μM (IC50)
CDK9/cyclinT1
>20 μM (IC50)
体外研究 (In Vitro)
CDK12-IN-6 (Example 174) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.872 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-6 has antproliferative activity in MDA-MB-231 cells (IC50=2.19 nM) and CAL-120 cells (IC50=1 nM)[1]. CDK12-IN-6 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 1851[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
425.44
Formula
C20H21F2N9
CAS 号
2651196-71-1
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.
CDK12-IN-5 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 23.9 nM。CDK12-IN-5 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50=173 μM) 和 CDK9/Cyclin T1 (IC50=127 μM) 没有影响(WO2021116178A1)。
CDK12-IN-5 Chemical Structure
CAS No. : 2651200-35-8
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
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1)[1].
IC50 & Target[1]
CDK12
23.9 nM (IC50)
CDK2/cyclinE
173 μM (IC50)
CDK9/cyclinT1
127 μM (IC50)
体外研究 (In Vitro)
CDK12-IN-5 (Example 426) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=3.23 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-5 has antproliferative activity in MDA-MB-231 cells (IC50=4.19 nM) and CAL-120 cells (IC50=3.57 nM)[1]. CDK12-IN-5 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 32[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
454.36
Formula
C18H15F5N8O
CAS 号
2651200-35-8
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.
CDK12-IN-4 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 0.641 μM。CDK12-IN-4 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50>20 μM) 和 CDK9/Cyclin T1 (IC50>20 μM) 没有影响(WO2021116178A1)。
CDK12-IN-4 Chemical Structure
CAS No. : 2651196-69-7
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
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1)[1].
IC50 & Target[1]
CDK12
0.641 μM (IC50)
CDK2/cyclinE
>20 μM (IC50)
CDK9/cyclinT1
>20 μM (IC50)
体外研究 (In Vitro)
CDK12-IN-4 (Example 172) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.626 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-4 has antproliferative activity in MDA-MB-231 cells (IC50=0.535 nM) and CAL-120 cells (IC50=2.43 nM)[1]. CDK12-IN-4 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 581[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
426.42
Formula
C20H20F2N8O
CAS 号
2651196-69-7
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.
CDK12-IN-6 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 1.19 μM。CDK12-IN-6 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50>20 μM) 和 CDK9/Cyclin T1 (IC50>20 μM) 没有影响(WO2021116178A1)。
CDK12-IN-6 Chemical Structure
CAS No. : 2651196-71-1
规格
是否有货
5 mg
询价
10 mg
询价
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
生物活性
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1)[1].
IC50 & Target[1]
CDK12
1.19 μM (IC50)
CDK2/cyclinE
>20 μM (IC50)
CDK9/cyclinT1
>20 μM (IC50)
体外研究 (In Vitro)
CDK12-IN-6 (Example 174) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.872 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-6 has antproliferative activity in MDA-MB-231 cells (IC50=2.19 nM) and CAL-120 cells (IC50=1 nM)[1]. CDK12-IN-6 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 1851[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
425.44
Formula
C20H21F2N9
CAS 号
2651196-71-1
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.
CDK12-IN-5 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 23.9 nM。CDK12-IN-5 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50=173 μM) 和 CDK9/Cyclin T1 (IC50=127 μM) 没有影响(WO2021116178A1)。
CDK12-IN-5 Chemical Structure
CAS No. : 2651200-35-8
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
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1)[1].
IC50 & Target[1]
CDK12
23.9 nM (IC50)
CDK2/cyclinE
173 μM (IC50)
CDK9/cyclinT1
127 μM (IC50)
体外研究 (In Vitro)
CDK12-IN-5 (Example 426) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=3.23 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-5 has antproliferative activity in MDA-MB-231 cells (IC50=4.19 nM) and CAL-120 cells (IC50=3.57 nM)[1]. CDK12-IN-5 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 32[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
454.36
Formula
C18H15F5N8O
CAS 号
2651200-35-8
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.
CDK12-IN-4 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 0.641 μM。CDK12-IN-4 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50>20 μM) 和 CDK9/Cyclin T1 (IC50>20 μM) 没有影响(WO2021116178A1)。
CDK12-IN-4 Chemical Structure
CAS No. : 2651196-69-7
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
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1)[1].
IC50 & Target[1]
CDK12
0.641 μM (IC50)
CDK2/cyclinE
>20 μM (IC50)
CDK9/cyclinT1
>20 μM (IC50)
体外研究 (In Vitro)
CDK12-IN-4 (Example 172) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.626 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-4 has antproliferative activity in MDA-MB-231 cells (IC50=0.535 nM) and CAL-120 cells (IC50=2.43 nM)[1]. CDK12-IN-4 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 581[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
426.42
Formula
C20H20F2N8O
CAS 号
2651196-69-7
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.
CDK12-IN-6 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 1.19 μM。CDK12-IN-6 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50>20 μM) 和 CDK9/Cyclin T1 (IC50>20 μM) 没有影响(WO2021116178A1)。
CDK12-IN-6 Chemical Structure
CAS No. : 2651196-71-1
规格
是否有货
5 mg
询价
10 mg
询价
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
生物活性
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1)[1].
IC50 & Target[1]
CDK12
1.19 μM (IC50)
CDK2/cyclinE
>20 μM (IC50)
CDK9/cyclinT1
>20 μM (IC50)
体外研究 (In Vitro)
CDK12-IN-6 (Example 174) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.872 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-6 has antproliferative activity in MDA-MB-231 cells (IC50=2.19 nM) and CAL-120 cells (IC50=1 nM)[1]. CDK12-IN-6 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 1851[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
425.44
Formula
C20H21F2N9
CAS 号
2651196-71-1
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.
CDK12-IN-5 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 23.9 nM。CDK12-IN-5 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50=173 μM) 和 CDK9/Cyclin T1 (IC50=127 μM) 没有影响(WO2021116178A1)。
CDK12-IN-5 Chemical Structure
CAS No. : 2651200-35-8
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
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1)[1].
IC50 & Target[1]
CDK12
23.9 nM (IC50)
CDK2/cyclinE
173 μM (IC50)
CDK9/cyclinT1
127 μM (IC50)
体外研究 (In Vitro)
CDK12-IN-5 (Example 426) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=3.23 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-5 has antproliferative activity in MDA-MB-231 cells (IC50=4.19 nM) and CAL-120 cells (IC50=3.57 nM)[1]. CDK12-IN-5 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 32[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
454.36
Formula
C18H15F5N8O
CAS 号
2651200-35-8
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.
CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor with Kis of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively[1]. (from patent WO2019207463A1 example A93).
体外研究 (In Vitro)
The CDK4 and CDK6 cell-based IC50s of CDK4/6-IN-5 in JEKO-1 and MV4-1 1 cells are 23.8 and 61.4 nM, respectively[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
527.01
Formula
C22H28ClFN6O4S
CAS 号
2380321-50-4
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]. Ping Chen, et al. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors. WO2019207463A1.
CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor with Kis of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively[1]. (from patent WO2019207463A1 example A93).
体外研究 (In Vitro)
The CDK4 and CDK6 cell-based IC50s of CDK4/6-IN-5 in JEKO-1 and MV4-1 1 cells are 23.8 and 61.4 nM, respectively[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
527.01
Formula
C22H28ClFN6O4S
CAS 号
2380321-50-4
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]. Ping Chen, et al. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors. WO2019207463A1.
