SCH900776 | MK-8776 | CHK1 Inhibitor | AmBeed-信号通路专用抑制剂

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SCH900776 {[allProObj[0].p_purity_real_show]}

货号：A200833 同义名： MK-8776

SCH 900776 (MK-8776) is a selective and highly potent CHK1 inhibitor with IC50 value of 3nM, modest to CDK2 and Chk2 with much higher IC50 values of 160nM and 1.5uM, respectively.

SCH900776 化学结构
CAS号：891494-63-6

SCH900776 3D分子结构
CAS号：891494-63-6

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SCH900776 纯度/质量文件产品仅供科研

货号：A200833 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

Chk 亚型比较
CDK 亚型比较

产品名称	Chk1 ↓ ↑	Chk2 ↓ ↑	其他靶点	纯度
Rabusertib	++ Chk1, IC50: 7 nM			99%+
PF-477736	++++ Chk1, Ki: 0.49 nM			98%+
Prexasertib 2HCl	++++ Chk1, Ki: 0.9 nM	++ Chk2, IC50: 8 nM	RSK	98%
AZD-7762	+++ Chk1, IC50: 5 nM	++ Chk2, IC50: <10 nM		99%+
CHIR-124	++++ Chk1, IC50: 0.3 nM		FLT3,PDGFR,GSK-3	98%
SCH900776	+++ Chk1, IC50: 3 nM			99%+
SAR-020106	+ Chk1, IC50: 13.3 nM			98%
CCT245737	+++ Chk1, IC50: 1.4 nM			97+%
BML-277		+ Chk2, 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。

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ 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/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 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	98%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 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/CyclinE, IC50: 8 nM CDK2/CyclinA, 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/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 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 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	98%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, 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 dihydrochloride									++++ 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				98+%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			99+%
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												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 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。

SCH900776 生物活性

靶点	CDK2 CDK2, IC50:0.16 μM Chk1 Chk1, IC50:3 nM
描述	Chk1 (Checkpoint kinase 1), an important serine/threonine kinase, is responding to DNA damage and stall DNA replication. Chk1 plays a key role in maintaining the replication fork viability during exposure to DNA antimetabolites. Inhibition of Chk1 will lead to accumulation of double-strand DNA breaks and cell death in human tumor cell lines exposure to anti-metabolite. SCH 900776 (MK-8776) is a selective and highly potent CHK1 inhibitor with IC50 value of 3 nM (measured by kinase assays), modest to CDK2 and Chk2 with much higher IC50 values of 160 nM and 1.5 μM, respectively. Treatment with 8 - 500 nM of SCH 900776 for 2h led to dose-dependent accumulation of DNA double-strand breaks induced by hydroxyurea in U2OS cells (measured by g-H2AX, a biomarker of DNA double-strand breaks). Consistent with that, 0.06 – 2 μM SCH 900776 for 2h caused decreased level of p-Ser296 site of Chk1 (an autophosphorylation site of Chk1) in U2OS cells exposure to hydroxyurea. SCH 900776 can induce a dose-dependent loss of DNA replication capability (measured by BrdU positive cells number) after the hydroxyurea exposure. An increase in the sub-G1 population was also observed, suggesting the cell death within the culture. Consistent with that, SCH 900776 exposure can enhance apoptosis for at least 48h following release from hydroxyurea blockade. Intraperitoneally injection of 8 - 32 mg/kg SCH-900776, 30 minutes after gemcitabine (150 mg/kg) 3 cycles of treatment on every fifth day, can lead to enhanced tumor pharmacodynamic and regression responses relative to either agent alone in the A2780 xenografted models^[1]. Up to now, a phase I study of SCH-900776 in combination with gemcitabine in solid tumours and lymphoma has been completed^[2].
作用机制	SCH-900776 is an ATP competitive inhibitor^[2].

SCH900776 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A2058	37.5-300 nM	Cell Viability Assay	72 h	reduces the MK-1775 EC50 by 5-fold to an average of 45 nM	23148684
A498	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
AsPC-1	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
AsPC-1	10-1000 nM	Growth Inhibition Assay	24-48h	enhances the chemosensitization to gemcitabine	23804422

SCH900776 动物研究

Dose

Mice^[1] (i.p.): min = 4 mg/kg, max = 50 mg/kg

Administration

i.p.

Pharmacokinetics

Animal	Nude mice^[1]
Dose	10 - 100 (mg/kg)
Administration	i.p.
C_max	0.56 - 19 (μM)
T_max	1 h
AUC	0.9 - 57 (μM·hr)

SCH900776 参考文献

[1]Guzi TJ, Paruch K, et al. Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. Mol Cancer Ther. 2011 Apr;10(4):591-602.

[2]Matthews TP, Jones AM, et al. Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies. Expert Opin Drug Discov. 2013 Jun;8(6):621-40.

SCH900776 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.29mL

2.66mL

1.33mL

26.58mL

5.32mL

2.66mL

SCH900776 技术信息

CAS号	891494-63-6
分子式	C₁₅H₁₈BrN₇
分子量	376.254

别名	MK-8776
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 105 mg/mL(279.07 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

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

A2058	37.5-300 nM	Cell Viability Assay	72 h	reduces the MK-1775 EC50 by 5-fold to an average of 45 nM	23148684
A498	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
AsPC-1	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
AsPC-1	10-1000 nM	Growth Inhibition Assay	24-48h	enhances the chemosensitization to gemcitabine	23804422
BxPC-3	10-1000 nM	Growth Inhibition Assay	24-48h	enhances the chemosensitization to gemcitabine	23804422
H1299	500 nM	Growth Inhibition Assay	24 h	enhances the chemosensitization to PMX	24113549
H1437	500 nM	Growth Inhibition Assay	24 h	enhances the chemosensitization to PMX	24113549
H1993	500 nM	Growth Inhibition Assay	24 h	enhances the chemosensitization to PMX	24113549
H2009	500 nM	Cell Viability Assay	72 h	results in G1/S-phase accumulation combined with MK-1775	23148684
H23	500 nM	Growth Inhibition Assay	24 h	enhances the chemosensitization to PMX	24113549
HCC2998	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
HCT115	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
HCT116	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
HCT116	1 µM	Function Assay	24 h	abrogates of cell cycle arrest	22510560
HL-60	30/100/300 nM	Apoptosis Assay	24 h	enhances cytarabine-induced apoptosis	22869869
HMEC	500 nM	Cell Viability Assay	72 h	results in G1/S-phase accumulation combined with MK-1775	23148684
HRE	500 nM	Cell Viability Assay	72 h	results in G1/S-phase accumulation combined with MK-1775	23148684
IGROV-1	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
MCF10A	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
MDA-MB-231	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
MDA-MB-435	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
MiaPaCa-2	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
MiaPaCa-2	10-1000 nM	Growth Inhibition Assay	24-48h	enhances the chemosensitization to gemcitabine	23804422
ML-1	25/50/100 nM	Apoptosis Assay	24 h	enhances cytarabine-induced apoptosis	22869869
MOLM-13	100-700 nM	Apoptosis Assay	48 h	induces apoptosis dose dependently	23536721
MV-4-11	100-700 nM	Apoptosis Assay	48 h	induces apoptosis dose dependently	23536721
OVCAR-8	0.3 µM	Growth Inhibition Assay	8 d	sensitizes the cell lines to gemcitabine	23548269
SKOV3	0.3 µM	Growth Inhibition Assay	8 d	sensitizes the cell lines to gemcitabine	23548269
SNB19	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
Su.86.86	500 nM	Cell Viability Assay	72 h	results in G1/S-phase accumulation combined with MK-1775	23148684
SW620	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
TK10	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
U20S	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
U251	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
U2OS	2 µM	Function Assay	0-24 h	induces phosphorylation of Chk1 at serine 345 at both concentrations as early as 2 h after administration	22937147
U2OS	0-10 µM	Growth Inhibition Assay	24/48 h	inhibits cell growth dose dependently	22937147
U2OS	1 µM	Function Assay	24 h	abrogates of cell cycle arrest	22510560
U87	200/2000 nM	Growth Inhibition Assay	24 h	decreases the IC50 of Gemcitabine	24359526
U937	100-700 nM	Apoptosis Assay	48 h	induces apoptosis dose dependently	23536721
U937	100-500 nM	Function Assay	4 h	decreases the cytarabine-induced Chk1 autophosphorylation at Ser296 and prevents Cdc25A downregulation	22869869
U937	100 nM	Function Assay	4 h	reverses the cytarabine-induced inhibition of 3H-thymidine incorporation into DNA	22869869
U937	100-500 nM	Function Assay	4 h	induces increased phosphorylation of H2AX	22869869

SCH900776 {[allProObj[0].p_purity_real_show]}

SCH900776 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

SCH900776 质控信息

SCH900776 生物活性

SCH900776 细胞研究

SCH900776 动物研究

SCH900776 参考文献

SCH900776 实验方案

SCH900776 技术信息

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SCH900776 纯度/质量文件 产品仅供科研

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