377090-84-1|SU 9516|SU 9516|MFCD05865243-范德生物科技公司

SU 9516

NMR下载 COA and HPLC MSDS下载
names：
SU 9516
CAS号：
377090-84-1
MDL Number： MFCD05865243
MF(分子式)： C13H11N3O2 MW(分子量)： 241.245
EINECS: Reaxys Number:
Pubchem ID:5289419 Brand:BIOFOUNT

SU 9516(377090-84-1)是一种有效的选择性cdk2抑制剂（对于cdk2，cdk1，cdk4，PKC，p38，PDGFR和EGFR，IC50值分别为0.022、0.04，> 10，> 10、18和> 100μM）。抑制pRb磷酸化，导致增强的pRB / E2F复合物形成，并诱导G1和G2-M细胞周期停滞。转录下调Mcl-1，并在体外具有抗增殖，抑制细胞生长和促凋亡作用。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
HCC345388-5mg	5mg	97%	¥ 2992.50	¥ 2992.50		4-7周	- +	¥ 0.00

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中文别名	SU 9516(377090-84-1);SU-9516;SU 9516;SU9516;3-（1-（3H-咪唑-4-基）-甲基-（Z）-亚烷基）-5-甲氧基-1,3-二氢-吲哚-2-一;
英文别名	SU 9516(377090-84-1);SU-9516;SU 9516;SU9516;3-(1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene)-5-methoxy-1,3-dihydro-indol-2-one;
CAS号	377090-84-1
Inchi	InChI=1S/C13H11N3O2/c1-18-9-2-3-12-10(5-9)11(13(17)16-12)4-8-6-14-7-15-8/h2-7H,1H3,(H,14,15)(H,16,17)/b11-4-
InchiKey	QNUKRWAIZMBVCU-WCIBSUBMSA-N
分子式 Formula	C13H11N3O2
分子量 Molecular Weight	241.245
溶解度Solubility	生物体外In Vitro:DMSO溶解度≥ 100 mg/mL(414.51 mM)H2O< 0.1 mg/mL(insoluble)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性状	棕色结晶的固体粉末
储藏条件 Storage conditions	Store at +4°C，storage at -4℃ (1-2weeks), longer storage period at -20℃ (1-2years)

SU 9516(377090-84-1)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.

Tags:SU 9516试剂,SU 9516杂质,SU 9516中间体,SU 9516密度,SU 9516溶解度,SU 9516旋光度,SU 9516闪点,SU 9516熔点,SU 9516购买,SU 9516结构式,

产品说明	SU 9516(377090-84-1)可以作为药物杂质对照品以及生物医药类试剂。
Introduction	SU 9516(377090-84-1) can be used as a reference substance for drug impurities and reagents，only for research.
Application1	SU9516是一种有效的CDK2抑制剂，IC50约为22 nM，同时对CDK1和CDK4也有抑制作用，IC50 值分别为40和200 nM。
Application2
Application3

SU 9516(377090-84-1)药理学：

SU 9516是一种有效的选择性cdk2抑制剂（对于cdk2，cdk1，cdk4，PKC，p38，PDGFR和EGFR，IC50值分别为0.022、0.04，> 10，> 10、18和> 100μM）。抑制pRb磷酸化，导致增强的pRB / E2F复合物形成，并诱导G1和G2-M细胞周期停滞。转录下调Mcl-1，并在体外具有抗增殖，抑制细胞生长和促凋亡作用。

SU-9516是选择性CDK2抑制剂，IC50为22 nM；对CDK1 / CDK4的效力较低（IC50 = 40/200 nM），对PKC，EGFR，p38MAPK等无抑制作用；IC50值：22 nM / 40 nM（CDK2 / CDK1）[1]；目标：CDK2抑制剂；体外：SU9516是cdk 2的有效抑制剂，对cdk2的选择性分别是cdk4和cdk1的9倍和1.8倍。对CDK1 / CDK4的效力较低（IC50 = 40/200 nM），对PKC，EGFR，p38MAPK等无抑制作用。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303+H313+H333
安全防护	P264+P280+P305+P351+P338+P337+P313
备注	实验过程中防止吸入、食入，做好安全防护

Degterev et al..Identification of RIP1 kinase as a specific cellular target of necrostatins,Nature Chemical Biology, 2008[DOI: 10.1038nchembio.83]

Rescifina Antonio, Scala Angela, Sciortino Maria Teresa, Colao Ivana, Siracusano Gabriel, Mazzaglia Antonino, Chiacchio Ugo, Grassi Giovanni.Decorated 6,6′,7,7′-tetrahydro-1H,1′H-2,3′-biindole scaffold as promising candidate for recognition of the CDK2 allosteric site,Med. Chem. Commun., 2014[DOI: 10.1039C4MD00364K]

Lane ME, et al. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 2001 Aug 15;61(16):6170-7.

Yu B, et al. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochem Pharmacol. 2002 Oct 1;64(7):1091-100.

Gao N, et al. The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via d

SU 9516(377090-84-1)参考文献：

1.Cyclin-dependent kinase inhibitor SU9516 enhances sensitivity to methotrexate in human T-cell leukemia Jurkat cells.
Uchiyama H1, Sowa Y, Wakada M, Yogosawa M, Nakanishi R, Horinaka M, Shimazaki C, Taniwaki M, Sakai T. Cancer Sci. 2010 Mar;101(3):728-34. doi: 10.1111/j.1349-7006.2009.01449.x. Epub 2009 Nov 27.

Methotrexate (MTX) has been used to treat various hematological malignancies. Since MTX prevents tumor cells from proliferating by inhibiting dihydrofolate reductase (DHFR), DHFR expression is a key determinant of resistance to MTX in malignant hematological tumor cells. The antiproliferative effect of MTX was significantly enhanced by the knockdown of DHFR expression by siRNA in Jurkat cells. Therefore, a novel strategy down-regulating DHFR expression seems promising for enhancing sensitivity to MTX. We found that SU9516, a cyclin-dependent kinase inhibitor, reduced the expression of both DHFR mRNA and protein. Moreover, we found that DHFR promoter activity was attenuated by SU9516 dependent on the E2F site. Finally, pretreatment with SU9516 significantly enhanced sensitivity to MTX in a colony formation assay. We conclude that a combination of cyclin-dependent kinase inhibitors and MTX may be useful for overcoming resistance to MTX.

2.The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional mechanism.
Gao N1, Kramer L, Rahmani M, Dent P, Grant S. Mol Pharmacol. 2006 Aug;70(2):645-55. Epub 2006 May 3.

Mechanisms of lethality of the three-substituted indolinone and putatively selective cyclin-dependent kinase (CDK)2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) were examined in human leukemia cells. Exposure of U937 and other leukemia cells to SU9516 concentrations > or =5 microM rapidly (i.e., within 4 h) induced cytochrome c release, Bax mitochondrial translocation, and apoptosis in association with pronounced down-regulation of the antiapoptotic protein Mcl-1. These effects were associated with inhibition of phosphorylation of the carboxyl-terminal domain (CTD) of RNA polymerase (Pol) II on serine 2 but not serine 5. Reverse transcription-polymerase chain reaction analysis revealed pronounced down-regulation of Mcl-1 mRNA levels in SU9516-treated cells. Similar results were obtained in Jurkat and HL-60 leukemia cells. Furthermore, cotreatment with the proteasome inhibitor N-benzoyloxycarbonyl (Z)-Leu-Leu-leucinal (MG132) blocked SU9516-mediated Mcl-1 down-regulation, implicating proteasomal degradation in diminished expression of this protein.

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