942425-68-5|PHA-767491盐酸盐|PHA-767491 hydrochloride|MFCD11519962-范德生物科技公司

PHA-767491盐酸盐

NMR下载 COA and HPLC MSDS下载
names：
PHA-767491 hydrochloride
CAS号：
942425-68-5
MDL Number： MFCD11519962
MF(分子式)： C12H12ClN3O MW(分子量)： 249.7
EINECS: Reaxys Number:
Pubchem ID:11715766 Brand:BIOFOUNT

PHA-767491盐酸盐(942425-68-5,PHA-767491 hydrochloride,CAY-10572 hydrochloride)是一种有效的，具有ATP竞争性的双重Cdc7 / Cdk9抑制剂，可防止DNA复制的开始。它在多种人类细胞系中抑制细胞增殖，并在体内以p53独立的方式诱导细胞凋亡。它还抑制有丝分裂原激活的蛋白激酶激活的蛋白激酶2（MK2）。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
YZM001253-50mg	50mg	99.91%	¥ 2761.00	¥ 2761.00		2-3天	- +	¥ 0.00
YZM001253-10mg	10mg	99.91%	¥ 646.43	¥ 646.43		2-3天	- +	¥ 0.00

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中文别名	PHA-767491盐酸盐(942425-68-5); CAY-10572盐酸盐；PHA-767491盐酸盐；CAY 10572盐酸盐；PHA 767491盐酸盐；CAY10572盐酸盐；PHA767491盐酸盐;
英文别名	PHA-767491 hydrochloride(942425-68-5);CAY-10572 hydrochloride; PHA-767491 hydrochloride; CAY 10572 hydrochloride; PHA 767491 hydrochloride; CAY10572 hydrochloride; PHA767491 hydrochloride;
CAS号	942425-68-5
SMILES	O=C1C2=C(NC(C3=CC=NC=C3)=C2)CCN1.[H]Cl
Inchi	InChI=1S/C12H11N3O.ClH/c16-12-9-7-11(8-1-4-13-5-2-8)15-10(9)3-6-14-12;/h1-2,4-5,7,15H,3,6H2,(H,14,16);1H
InchiKey	IMVNFURYBZMFDZ-UHFFFAOYSA-N
分子式 Formula	C12H12ClN3O
分子量 Molecular Weight	249.7
闪点 FP
熔点 Melting point	No data available
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility	生物体外In Vitro:H2O : 50 mg/mL(200.24 mM;Need ultrasonic)DMSO溶解度17.33 mg/mL(69.40 mM;Need ultrasonic and warming)
性状	固体粉末,Power
储藏条件 Storage conditions	-20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

PHA-767491盐酸盐(942425-68-5,PHA-767491 hydrochloride,CAY-10572 hydrochloride)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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产品说明	PHA-767491盐酸盐(942425-68-5,PHA-767491 hydrochloride,CAY-10572 hydrochloride)是一种有效的Cdc7-Dbf4(DDK)/Cdk9的双重的抑制剂
Introduction	PHA-767491盐酸盐(942425-68-5,PHA-767491 hydrochloride,CAY-10572 hydrochloride)is a dualCdc7/Cdk9inhibitor, withIC50s of 10 nM and 34 nM, respectively.
Application1	PHA-767491 hydrochloride 是一种 Cdc7-Dbf4 (DDK)/Cdk9 的双重抑制剂，IC50 值分别为 10 nM 和 34 nM。
Application2	ATP竞争性强的双重cdc7 / cdk9抑制剂（IC50值分别为10和34 nM），可防止DNA复制的启动。在体内抑制多种人类细胞系（IC50?0.86- 5.87 muM）中的细胞增殖，并诱导细胞凋亡。还抑制促分裂原激活的蛋白激酶激活的蛋白激酶2（MK2）（IC50 = 171 nM）。
Application3

PHA-767491盐酸盐(942425-68-5,PHA-767491 hydrochloride,CAY-10572 hydrochloride)药理学：

PHA-767491盐酸盐是一种有效的，具有ATP竞争性的双重Cdc7 / Cdk9抑制剂，可防止DNA复制的开始。它在多种人类细胞系中抑制细胞增殖，并在体内以p53独立的方式诱导细胞凋亡。它还抑制有丝分裂原激活的蛋白激酶激活的蛋白激酶2（MK2）。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

Sasi NK, et al. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One. 2014 Nov 20;9(11):e11

Li W, et al. Dual Inhibition of Cdc7 and Cdk9 by PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. Curr Cancer Drug Targets. 2015;15(3):196-204.

Erbayraktar Z, et al. Cell division cycle 7-kinase inhibitor PHA-767491 hydrochloride suppresses glioblastoma growth and invasiveness. Cancer Cell Int. 2016 Nov 18;16:88.

Montagnoli A, et al. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65.

PHA-767491盐酸盐(942425-68-5,PHA-767491 hydrochloride,CAY-10572 hydrochloride)参考文献：

1、Structure-function study of a novel inhibitor of the casein kinase 1 family in Arabidopsis thaliana
Ami N Saito 1, Hiromi Matsuo 2, Keiko Kuwata 2, Azusa Ono 3, Toshinori Kinoshita 2 3, Junichiro Yamaguchi 1, Norihito Nakamich

Abstract Casein kinase 1 (CK1) is an evolutionarily conserved protein kinase family among eukaryotes. Studies in non-plants have shown CK1-dependent divergent biological processes, but the collective knowledge regarding the biological roles of plant CK1 lags far behind other members of the Eukarya. One reason for this is that plants have many more genes encoding CK1 than do animals. To accelerate our understanding of the plant CK1 family, a strong CK1 inhibitor that efficiently inhibits multiple members of the CK1 protein family in vivo (i.e., in planta) is required. Here, we report a novel, specific, and effective CK1 inhibitor in Arabidopsis. Using circadian period-lengthening activity as an estimation of the CK1 inhibitor effect in vivo, we performed a structure-activity relationship study of analogues of the CK1 inhibitor PHA767491 (1,5,6,7-tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride). A propargyl group at the pyrrole nitrogen atom (AMI-212) or a bromine atom at the pyrrole C3 position (AMI-23) had stronger CK1 inhibitory activity than PHA767491. A hybrid molecule of AMI-212 and AMI-23 (AMI-331) was about 100-fold more inhibitory than the parent molecule PHA767491. Affinity proteomics using an AMI-331 probe showed that the targets of AMI-331 inhibition are mostly CK1 kinases. As such, AMI-331 is a potent and selective CK1 inhibitor that shows promise in the research of CK1 in plants.

2、Cell division cycle 7-kinase inhibitor PHA-767491 hydrochloride suppresses glioblastoma growth and invasiveness
Zubeyde Erbayraktar # 1, Begum Alural # 2 3, Resat Serhat Erbayraktar 4, Erdogan Pekcan Erkan

Abstract Background: Genomic instability is a hallmark of cancer cells, and this cellular phenomenon can emerge as a result of replicative stress. It is possible to take advantage of replicative stress, and enhance it in a targeted way to fight cancer cells. One of such strategies involves targeting the cell division cycle 7-related protein kinase (CDC7), a protein with key roles in regulation of initiation of DNA replication. CDC7 overexpression is present in different cancers, and small molecule inhibitors of the CDC7 have well-documented anti-tumor effects. Here, we aimed to test the potential of CDC7 inhibition as a new strategy for glioblastoma treatment. Methods: PHA-767491 hydrochloride was used as the CDC7 inhibitor. Two glioblastoma cell lines (U87-MG and U251-MG) and a control cell line (3T3) were used to characterize the effects of CDC7 inhibition. The effect of CDC7 inhibition on cell viability, cell proliferation, apoptosis, migration, and invasion were analyzed. In addition, real-time PCR arrays were used to identify the differentially expressed genes in response to CDC7 inhibition. Results: Our results showed that CDC7 inhibition reduces glioblastoma cell viability, suppresses cell proliferation, and triggers apoptosis in glioblastoma cell lines. In addition, we determined that CDC7 inhibition also suppresses glioblastoma cell migration and invasion. To identify molecular targets of CDC7 inhibition, we used real-time PCR arrays, which showed dysregulation of several mRNAs and miRNAs. Conclusions: Taken together, our findings suggest that CDC7 inhibition is a promising strategy for treatment of glioblastoma.

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