LDC4297 | LDC044297 | CDK7 Inhibitor | AmBeed-信号通路专用抑制剂

LDC4297 {[allProObj[0].p_purity_real_show]}

货号：A162429 同义名： LDC044297

LDC4297 is a potent CDK7 selective inhibitor with IC50 of 0.13 ± 0.06 nM.

LDC4297 化学结构
CAS号：1453834-21-3

LDC4297 3D分子结构
CAS号：1453834-21-3

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CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 HCl	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											ERK,SGK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 HCl	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 2HCl									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			98%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

LDC4297 生物活性

靶点

CDK7

CDK7, IC50:0.13 nM

描述

Cyclin-dependent protein kinase 7 (CDK7) plays an important role in cellular metabolism and viability. LDC4297 is a selective CDK7 inhibitor with an IC50 value of 0.13±0.06nM. It dose-dependently inhibited the replication of human cytomegalovirus in primary human fibroblasts with an EC₅₀ value of 24.5±1.3nM. LDC4297 at 0.37μM reduced Rb expression in uninfected control cells at 24-h post-treatment. In a selection of human-pathogenic Alpha- and Gammaherpesvirinae, LDC4297 blocked virus replication with EC₅₀ values ranging from 0.02-1.21μM. The half-life of LDC4297 (p.o., a single dose of 100mg/kg) in CD1 mice was 1.6h and the time to a mean peak plasma concentration was 1,297.6ng/mL.^[3]

作用机制

LDC4297 is a CDK7 inhibitor with antiviral activity at low concentrations.^[3]

LDC4297 细胞实验

Cell Line Rhesus CMV-infected HFFs Guinea pig embryonic fibroblasts (GPEFs) Human foreskin fibroblasts (HFFs) ARPE-19 cells Mouse embryonic fibroblasts (MEF) Human foreskin fibroblasts (HFF) H1975 cells H460 cells Panc89 Mia-Paca2 MCF-7 DU4475 Hs-578T	Concentration	Treated Time	Description	References
Rhesus CMV-infected HFFs	0.018 µM	7 days	To evaluate the synergistic antiviral effect of LDC4297 with MBV in the RhCMV model. Results showed that the MBV + LDC4297 combination exhibited synergism in RhCMV.	Pharmaceutics. 2023 Nov 27;15(12):2680
Guinea pig embryonic fibroblasts (GPEFs)	0.044 µM	7 days	To evaluate the synergistic antiviral effect of LDC4297 with MBV in the GPCMV model. Results showed that the MBV + LDC4297 combination exhibited synergism in GPCMV.	Pharmaceutics. 2023 Nov 27;15(12):2680
Human foreskin fibroblasts (HFFs)	0.009 µM	7 days	To evaluate the synergistic anti-HCMV effect of LDC4297 with vCDK/pUL97 inhibitors such as MBV, Ax7396, Gö6976, and Vi7392. Results showed significant drug synergism in all four combinations.	Pharmaceutics. 2023 Nov 27;15(12):2680
ARPE-19 cells	0.07 μM	7 days	Evaluate the inhibitory effect of LDC4297 on HCMV TB40, showing broad-spectrum antiherpesviral activity at nanomolar concentrations.	Int J Mol Sci. 2021 Jan 8;22(2):575
Mouse embryonic fibroblasts (MEF)	0.07 μM	5 days	Evaluate the inhibitory effect of LDC4297 on MCMV, showing broad-spectrum antiherpesviral activity at nanomolar concentrations.	Int J Mol Sci. 2021 Jan 8;22(2):575
Human foreskin fibroblasts (HFF)	0.02 μM	7 days	Evaluate the inhibitory effect of LDC4297 on HCMV, showing broad-spectrum antiherpesviral activity at nanomolar concentrations.	Int J Mol Sci. 2021 Jan 8;22(2):575
H1975 cells	10 μM	24 hours	LDC4297 significantly decreased glucose consumption and GLUT1 mRNA and protein levels in H1975 cells	Nat Commun. 2019 Nov 29;10(1):5444
H460 cells	10 μM	24 hours	LDC4297 significantly decreased glucose consumption and GLUT1 mRNA and protein levels in H460 cells	Nat Commun. 2019 Nov 29;10(1):5444
Panc89	0.05-0.3 μM	3 days	To evaluate the effect of LDC4297 on the viability of pancreatic cancer cells, results showed that Panc89 cells exhibited significantly higher sensitivity to LDC4297.	Int J Mol Sci. 2022 Jan 12;23(2):812
Mia-Paca2	0.05-0.3 μM	3 days	To evaluate the effect of LDC4297 on the viability of pancreatic cancer cells, results showed that Mia-Paca2 cells exhibited intermediate to good sensitivity at low concentrations of LDC4297.	Int J Mol Sci. 2022 Jan 12;23(2):812
MCF-7	2.5 and 5 uM	48 hours	LDC4297 treatment did not influence the expression of wild-type p53 in ER-positive breast cancer cells	Front Oncol. 2021 May 24;11:664848
DU4475	2.5 and 5 uM	48 hours	LDC4297 treatment did not influence the expression of wild-type p53 in TNBC cells	Front Oncol. 2021 May 24;11:664848
Hs-578T	2.5 and 5 uM	48 hours	LDC4297 treatment effectively downregulated p53 expression in TNBC cells with mutant-type p53	Front Oncol. 2021 May 24;11:664848

Cell Line

Concentration

Treated Time

Description

References

Rhesus CMV-infected HFFs

0.018 µM

7 days

To evaluate the synergistic antiviral effect of LDC4297 with MBV in the RhCMV model. Results showed that the MBV + LDC4297 combination exhibited synergism in RhCMV.

Pharmaceutics. 2023 Nov 27;15(12):2680

Guinea pig embryonic fibroblasts (GPEFs)

0.044 µM

7 days

To evaluate the synergistic antiviral effect of LDC4297 with MBV in the GPCMV model. Results showed that the MBV + LDC4297 combination exhibited synergism in GPCMV.

Pharmaceutics. 2023 Nov 27;15(12):2680

Human foreskin fibroblasts (HFFs)

0.009 µM

7 days

To evaluate the synergistic anti-HCMV effect of LDC4297 with vCDK/pUL97 inhibitors such as MBV, Ax7396, Gö6976, and Vi7392. Results showed significant drug synergism in all four combinations.

Pharmaceutics. 2023 Nov 27;15(12):2680

ARPE-19 cells

0.07 μM

7 days

Evaluate the inhibitory effect of LDC4297 on HCMV TB40, showing broad-spectrum antiherpesviral activity at nanomolar concentrations.

Int J Mol Sci. 2021 Jan 8;22(2):575

Mouse embryonic fibroblasts (MEF)

0.07 μM

5 days

Evaluate the inhibitory effect of LDC4297 on MCMV, showing broad-spectrum antiherpesviral activity at nanomolar concentrations.

Int J Mol Sci. 2021 Jan 8;22(2):575

Human foreskin fibroblasts (HFF)

0.02 μM

7 days

Evaluate the inhibitory effect of LDC4297 on HCMV, showing broad-spectrum antiherpesviral activity at nanomolar concentrations.

Int J Mol Sci. 2021 Jan 8;22(2):575

H1975 cells

10 μM

24 hours

LDC4297 significantly decreased glucose consumption and GLUT1 mRNA and protein levels in H1975 cells

Nat Commun. 2019 Nov 29;10(1):5444

H460 cells

10 μM

24 hours

LDC4297 significantly decreased glucose consumption and GLUT1 mRNA and protein levels in H460 cells

Nat Commun. 2019 Nov 29;10(1):5444

Panc89

0.05-0.3 μM

3 days

To evaluate the effect of LDC4297 on the viability of pancreatic cancer cells, results showed that Panc89 cells exhibited significantly higher sensitivity to LDC4297.

Int J Mol Sci. 2022 Jan 12;23(2):812

Mia-Paca2

0.05-0.3 μM

3 days

To evaluate the effect of LDC4297 on the viability of pancreatic cancer cells, results showed that Mia-Paca2 cells exhibited intermediate to good sensitivity at low concentrations of LDC4297.

Int J Mol Sci. 2022 Jan 12;23(2):812

MCF-7

2.5 and 5 uM

48 hours

LDC4297 treatment did not influence the expression of wild-type p53 in ER-positive breast cancer cells

Front Oncol. 2021 May 24;11:664848

DU4475

2.5 and 5 uM

48 hours

LDC4297 treatment did not influence the expression of wild-type p53 in TNBC cells

Front Oncol. 2021 May 24;11:664848

Hs-578T

2.5 and 5 uM

48 hours

LDC4297 treatment effectively downregulated p53 expression in TNBC cells with mutant-type p53

Front Oncol. 2021 May 24;11:664848

LDC4297 动物实验

Species Balb/c mice Balb/c mice	Animal Model Recombinant MCMV-UL97 infection model MCMV infection model	Administration	Dosage	Frequency	Description	References
Balb/c mice	Recombinant MCMV-UL97 infection model	Oral (p.o.)	LDC4297: 1 mg/kg/d; MBV: 0.1 mg/kg/d	Daily administration for 4 days	To evaluate the synergistic antiviral effect of MBV + LDC4297 in an in vivo model. Results showed significant synergism of the MBV + LDC4297 combination in vivo.	Pharmaceutics. 2023 Nov 27;15(12):2680
Balb/c mice	MCMV infection model	Oral gavage	20 mg/kg/d	Once daily for 5 days	Evaluate the in vivo inhibitory effect of LDC4297 on MCMV, showing significant reduction in viral load.	Int J Mol Sci. 2021 Jan 8;22(2):575

Species

Balb/c mice Balb/c mice

Animal Model

Recombinant MCMV-UL97 infection model MCMV infection model

Administration

Dosage

Frequency

Description

References

Balb/c mice

Recombinant MCMV-UL97 infection model

Oral (p.o.)

LDC4297: 1 mg/kg/d; MBV: 0.1 mg/kg/d

Daily administration for 4 days

To evaluate the synergistic antiviral effect of MBV + LDC4297 in an in vivo model. Results showed significant synergism of the MBV + LDC4297 combination in vivo.

Pharmaceutics. 2023 Nov 27;15(12):2680

Balb/c mice

MCMV infection model

Oral gavage

20 mg/kg/d

Once daily for 5 days

Evaluate the in vivo inhibitory effect of LDC4297 on MCMV, showing significant reduction in viral load.

Int J Mol Sci. 2021 Jan 8;22(2):575

LDC4297 参考文献

LDC4297 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL

LDC4297 技术信息

CAS号	1453834-21-3
分子式	C₂₃H₂₈N₈O
分子量	432.52
SMILES Code	CC(C1=C2N(N=C1)C(NCC3=CC=CC=C3N4N=CC=C4)=NC(OC5CNCCC5)=N2)C
MDL No.	MFCD28411427

别名	LDC044297
运输	蓝冰
InChI Key	LSGRZENCFIIHNV-UHFFFAOYSA-N
Pubchem ID	78161839

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 60 mg/mL(138.72 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

方案一

方案二

方案三

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