Silmitasertib (CX-4945)

For research use only. Not for use in humans.

目录号：S2248

Silmitasertib (CX-4945) Chemical Structure

CAS No. 1009820-21-6

Silmitasertib (CX-4945)是有效的，选择性CK2(casein kinase 2)抑制剂，无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。Silmitasertib可诱导自噬并促进细胞凋亡。Phase 1/2。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 2381.77	现货
2mg	RMB 1418.29	现货
5mg	RMB 2604.97	现货
50mg	RMB 7289.1	现货
100mg	RMB 10401.33	现货
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客户使用Selleck生产的Silmitasertib (CX-4945)发表文献91篇：

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Commun Biol, 2021, 4(1):638

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Cells, 2021, 10(2)338

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bioRxiv, 2021, 10.1101/2021.03.17.435124

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Nat Commun, 2020, 8;11(1):2289

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Diabetes, 2020, db191186

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Fertil Steril, 2020, 113(5):1067-1079.e5

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Curr Biol, 2020, S0960-9822(20)31413-5

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Transl Oncol, 2020, 13(1):70-78

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PLoS One, 2020, 15(1):e0227340

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Nat Struct Mol Biol, 2020, 27(1):92-104

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Mol Cell, 2019, 74(3):571-583

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Sci Adv, 2019, 5(8):eaav0318

PubMed: 31803841 ( click the link to review the publication )
EMBO J, 2019, 38(23):e101409

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Proc Natl Acad Sci U S A, 2019, 116(27):13374-13383

PubMed: 31209037 ( click the link to review the publication )

Cell Rep, 2019,

PubMed: 31825822 ( click the link to review the publication )

EBioMedicine, 2019, 49:106-117

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J Exp Clin Cancer Res, 2019, 18;38(1):131

PubMed: 30885251 ( click the link to review the publication )

Br J Cancer, 2019, 10.1038/s41416-019-0657-5

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Addict Biol, 2019, 10.1111/adb.12808

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Neurobiol Dis, 2019, 126:47-61

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Mol Cancer Res, 2019, 17(4):987-1001

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Cell Cycle, 2019, 18(24):3472-3490

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Oncol Rep, 2019, 10.3892/or.2019.7187

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Biomed Res Int, 2019, 2019:6125068

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Biol Res, 2019, 52(1):22

PubMed: 30992075 ( click the link to review the publication )

Int J Radiat Biol, 2019, 10.1080/09553002.2019.1642531

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Oncol Lett, 2019, 18(4):3845-3856

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Nucleic Acids Res, 2018, 46(10):5109-5124

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Oncogenesis, 2018, 7(11):84

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J Biol Chem, 2018, 293(8):2990-3002

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Biomed Pharmacother, 2018, 106:403-410

PubMed: 29966986 ( click the link to review the publication )

Biomed Pharmacother, 2018, 98:357-363

PubMed: 29275177 ( click the link to review the publication )

Biochemistry (Mosc), 2018, 83(11):1380-1387

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Anticancer Res, 2018, 38(11):6195-6200

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Nucleic Acids Res, 2018, 46(10):5050-5060

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Oncotarget, 2018, 9(102):37753-37765

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Oncotarget, 2018, 9(18):14597-14607

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Biochemistry (Moscow), 2018, 83-11

PubMed: None ( click the link to review the publication )

Cell Rep, 2017, 18(13):3167-3177

PubMed: 28355568 ( click the link to review the publication )

Exp Mol Med, 2017, 49(9):e375

PubMed: 28883547 ( click the link to review the publication )

Sci Rep, 2017, 7(1):16367

PubMed: 29180680 ( click the link to review the publication )

Cell Signal, 2017, 36:163-175

PubMed: 28487119 ( click the link to review the publication )

J Cell Biochem, 2017, 118(8):2463-2473

PubMed: 28133777 ( click the link to review the publication )

Pancreas, 2017, 46(4):575-581

PubMed: 28196025 ( click the link to review the publication )

PLoS ONE, 2017,

PubMed: 28542269 ( click the link to review the publication )

Heliyon, 2017, 3(6):e00318

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Pharmaceuticals (Basel), 2017, 10(1)E5

PubMed: 28045438 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2016, 113(36):10145-50

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Cancer Res, 2016, 76(9):2675-86

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J Cell Biol, 2016, 212(3):281-8

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Cell Signal, 2016, 28(2):23-31

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Oncotarget, 2016, 7(2):1323-40

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Pharmaceuticals (Basel), 2016, 10(1)E2

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Oncotarget, 2016, 7(18):26793-805

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eNeuro, 2016, 3(6)ENEURO.0092-16.2016

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Tumour Biol, 2016, 37(6):8293-304

PubMed: 26729194 ( click the link to review the publication )

Oncotarget, 2016, 7(52):87361-87372

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Nat Commun, 2015, 6:7227

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Cancer Lett, 2015, 356(2 Pt B):751-61

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Mol Cell Biochem, 2015, 404(1-2):103-12

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Advances in Biochemistry in Health and Disease, 2015, vol 12

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Cell Death Dis, 2014, 5:e1551

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Cell Signal, 2014, 26(12):2809-2817

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产品安全说明书

Casein Kinase抑制剂选择性比较

生物活性

产品描述

特性

CX-4945是促进人类临床实验的CK2的第一个口服生物相容性小分子抑制剂。

靶点

CK2 ^[1]
(Cell-free assay)

1 nM

体外研究

CX-4945是CK2特异的抑制剂，它只抑制238种激酶中的7种并且在0.5 μM浓度时它的抑制率超过90%，这是CK2的IC50的500多倍。虽然在无细胞系统中CX-4945抑制FLT3, PIM1和CDK1的IC50分别为35 nM, 46 nM和56 nM，但是在细胞基础上的功能实验中10 μM的CX-4945对FLT3, PIM1和 CDK1抑制作用不强。CX-4945有广谱的抗恶性细胞增生活性。乳腺癌细胞系对CX-4945敏感性最广泛，其EC50为1.71-20.01 μM。CX-4945的抗恶性细胞增生活性与CK2α mRNA和蛋白水平对应，但是与CK2α'催化亚基、调整CK2β亚族和PI3K/Akt 或 PTEN突变状态无关。CX-4945通过抑制CK2直接阻断Akt第129位丝氨酸的磷酸化作用来抑制PI3K/Akt信号通路，而不是通过抑制激活的PTEN起作用。用CX-4945处理可以引起磷酸化p21 (T145)减少，而p21和p27整体水平则会升高，同时诱导caspase 3/7活性。用CX-4945处理会诱导BT-474细胞阻断在细胞周期的G2/M期和BxPC-3细胞阻断在G1期。CX-4945会抑制HUVEC的增殖、迁移及血管新生，其IC50分别是5.5 μM, 2 μM和4 μM。在含氧量低的情况下BT-474和BxPC-3细胞用CX-4945处理，能阻断p53和pVHL下调，降低HIF-1α的转录活性^[1]。在Jurkat细胞中CX-4945能有效抑制内源细胞内的内源CK2的活性，其IC50是0.1 μM ^[2]。

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
A431	MVHGeY5kfGmxbjDBd5NigQ>?	MV6xNEDPxE1?	MoTQN\|AhdWmw		MVXheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p	NVjKWmRTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzPFc6QDhpPkKyN\|g4QTh6PD;hQi=>
H2170	M{LT[GZ2dmO2aX;uJGF{e2G7	NHvi[mgyOCEQvF2=	NHnmWXo{OCCvaX6=		MVzheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p	MnXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ\|OEe5PFgoRjJ{M{i3PVg5RC:jPh?=
A431	NIn2[mZHfW6ldHnvckBCe3OjeR?=	MX[xNEDPxE1?	MknnOE0zPCCq		M2LBVYVvcGGwY3XzJIFxd3C2b4Ppd{B4cXSqIHXycI91cW6rYh?=	M{niSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{i3PVg5Lz5{MkO4O\|k5QDxxYU6=
H2170	NEnISJNHfW6ldHnvckBCe3OjeR?=	NXHrdFlMOTBizszN	Mk[xOE0zPCCq		NV3aNmNF\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni	M{\jXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{i3PVg5Lz5{MkO4O\|k5QDxxYU6=
LNCap	NULCZ3NsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmLzNE0{OCEQvF2=	MoCzOEBl		MlHMTWM2OD12LkW5xsDPxE1?	M1PPNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OEOyN\|E3Lz5{MkizNlMyPjxxYU6=
A549	NUjweWhGT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3Tj[lAuOzBizszN	NWH2NZNNPzJiaB?=	MXnEUXNQ	NULzd5NpUUN3ME20MlE2KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=>	MonIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4NUG0OFMoRjJ\|NkWxOFQ{RC:jPh?=
H1299	NVmySJAyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3HJOlAuOzBizszN	NVi5UI1oPzJiaB?=	MVrEUXNQ	M4XRWWlEPTB;MT64NEDPxE1uIHnubIljcXS\|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm=	MknYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4NUG0OFMoRjJ\|NkWxOFQ{RC:jPh?=
A549	MY\GeY5kfGmxbjDBd5NigQ>?	MnL2NU8yOCEQvF2=	M{\4UVQ5KGh?	M4jBdmROW09?	MkW0cIVi\HNidH:gZUBld3OnLXTldIVv\GWwdDDk[YNz\WG\|ZTDpckBPd3SlaDDy[ZBwenSncjDhZ5Rqfmm2eR?=	NGrQO2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[1NVQ1Oyd-MkO2OVE1PDN:L3G+
S-LAMA84	MXXGeY5kfGmxbjDBd5NigQ>?	NVHYSm1{O8LizszN	Mn22NlQhcA>?	M3iyNGROW09?	NUm4eXVwemWmdXPld{BEUzJiYXP0bZZqfHl?	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDBzMkGwPUc,OjRyMUKxNFk9N2F-
R-LAMA84	NXvFTGZCTnWwY4Tpc44hSXO\|YYm=	MnrON:Kh\|ryP	NWXWeWFNOjRiaB?=	MmLUSG1UVw>?	MlT2doVlfWOnczDDT\|Ih[WO2aY\peJk>	M{DI[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEGyNVA6Lz5{NECxNlExQTxxYU6=
S-LAMA84	NWTiToN7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3qxSlIvPS1zMDFOwG0>	MWq0PEBp	MnruSG1UVw>?	MXzpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5	NXL0dXdvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNVIyODlpPkK0NFEzOTB7PD;hQi=>
R-LAMA84	MkjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlT5Nk42NTFyIN88US=>	M4rXR\|Q5KGh?	MXvEUXNQ	MX7pcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5	M2HyblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEGyNVA6Lz5{NECxNlExQTxxYU6=
A549	M2rTSGZ2dmO2aX;uJGF{e2G7	M3z4UVExKM7:TR?=	MYSxNk8zPC92ODDo		NEDGXoFqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgcYloemG2aX;uJIFv\CCrbo\hd4lwdg>?	NUm1XWdHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNlM6OzhpPkK0NFI{QTN6PD;hQi=>
A549	MVzGeY5kfGmxbjDBd5NigQ>?	MmLZN{DPxE1?	M4rlXlQ5KGh?		MVXpcohq[mm2czDUS2Yu\|rJzLXnu[JVk\WRiYXP0bZZifGmxbjDv[kBUdWGmIHHu[EBmgHC{ZYPzbY9vKG:oIGPuZYltKGGwZDDUe4l{fA>?	NHvMW5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECyN\|k{QCd-MkSwNlM6Ozh:L3G+
U-266	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NH3Gcm8xNTRyIN88US=>	Ml\SOFghcA>?		Mnv4TWM2OD1zOT64JOK2VcLi	M37zblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi2OFk1Lz5{NEC4OlQ6PDxxYU6=
INA-6	MnS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVuwMVQxKM7:TR?=	M2X3dFQ5KGh?		NXnS[25JUUN3ME2yMlQzKML3TR?=	NXmwemVGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFY1QTRpPkK0NFg3PDl2PD;hQi=>
Jeko-1	MoH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXOwMVQxKM7:TR?=	NVuzU5ZJPDhiaB?=		NIi3[5RKSzVyPUKuOEDDvU4EoB?=	M2rPNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi2OFk1Lz5{NEC4OlQ6PDxxYU6=
Rec-1	M{PjXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYqwMVQxKM7:TR?=	MYq0PEBp		NIXGRYxKSzVyPUGuOFYhyrWPwrC=	NEC2eVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4OlQ6PCd-MkSwPFY1QTR:L3G+
Jurkat	Mk\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVmxMVExKM7:TR?=	MY[0PEBp		NWHqfI9OUUN3ME20Mlkh\|ryP	Mn[0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NUOwNlQoRjJ2MkWzNFI1RC:jPh?=
CEM-R	M3PFNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVOxMVExKM7:TR?=	NFHmeoU1QCCq		NVPnRpB{UUN3ME20JO69VQ>?	NFm0eok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1N\|AzPCd-MkSyOVMxOjR:L3G+
CEM-S	NYnzZ\|d{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NE\LcoQyNTFyIN88US=>	MlvwOFghcA>?		Ml61TWM2OD12Lk[g{txO	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3M{CyOEc,OjR{NUOwNlQ9N2F-
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Jurkat	NEXG[WJHfW6ldHnvckBie3OjeR?=				MX;Jcohq[mm2aX;uJI9nKEONMjDpckBpfW2jbjDKeZJs[XRiY3XscJMh[XO\|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBc\2GvbXGzN3BeSVSSIHnuZ49zeG:{YYTpc44hcW62bzDzeYJ{fHKjdHWgZpkhdHWvaX7ld4NmdmOnIHHzd4F6NCCLQ{WwJF0hOC5zIN88UU4>	NV;BTHQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGxO\|Q1OzRpPkKxNVc1PDN2PD;hQi=>
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Jurkat	NYnpR3A{SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NGCxZ3c1KGSjeYO=		NH;EOm5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFr1dotifCClZXzsd{Bi\nSncjC0JIRigXNiYomgZYxidWG{IHLseYUh[XO\|YYmsJGlEPTBiPTCyMlUh\|ryPLh?=	NGPsd449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUG3OFQ{PCd-MkGxO\|Q1OzR:L3G+
A549	NHrzSGJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MoTDOEBl[Xm\|		MlTQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDNUS5JINmdGy\|IHHmeIVzKDRiZHH5d{BjgSCjbHHtZZIh[my3ZTDhd5NigSxiSVO1NEA:KDNizszNMi=>	NGXnRXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUG3OFQ{PCd-MkGxO\|Q1OzR:L3G+
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MV4-11	M{S4SWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MXOxJJRwKDNiZHH5dy=>		MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiBzIITvJFMh\GG7czDifUBOXFNiYYPzZZktKEOFNUCgQUA{KM7:TT6=	M4PvbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{GxPFMzLz5{M{exNVg{OjxxYU6=
U937	NHHIb21CdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NELVVHMyKHSxIEOg[IF6ew>?		M2rnZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVUmzO{Bk\WyuczDh[pRmeiBzIITvJFMh\GG7czDifUBOXFNiYYPzZZktKEOFNUCgQUA1NjJizszNMi=>	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzMUizNkc,OjN5MUG4N\|I9N2F-
Jurkat	Mm\FRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MX[xJJRwKDNiZHH5dy=>		MnPiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCMdYLrZZQh[2WubIOgZYZ1\XJiMTD0c{A{KGSjeYOgZpkhVVSVIHHzd4F6NCCFQ{WwJF0hPC53IN88UU4>	NImxXJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exNVg{Oid-MkO3NVE5OzJ:L3G+
K562	M331RmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MmLCNUB1dyB\|IHThfZM>		NUC4bXJESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEGgeI8hOyCmYYnzJIJ6KE2WUzDhd5NigSxiQ1O1NEA:KDdizszNMi=>	NITrb2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exNVg{Oid-MkO3NVE5OzJ:L3G+
Sf9	MnroSpVv[3Srb36gZZN{[Xl?				NVrpWYNYUW6qaXLpeIlwdiCxZjDDSGszN2O7Y3zpckBGKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGPmPUBk\WyuczD1d4lv\yCqaYP0c45mKEhzIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDb[4FudWF\|M2DdRXRRNCCLQ{WwJF0hOS56IN88UU4>	MoHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4OEG5PFYoRjJ2NkixPVg3RC:jPh?=
A549	M4DnSGN6fG:2b4jpZ4l1gSCjc4PhfS=>		NXHYUG44PzJiaILz		NFvYT3dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEOFNUCgQUA6NjlizszNMi=>	NIezb5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki1NFM4Pid-Mk[4OVA{PzZ:L3G+
Sf21	NVLjZnlDTnWwY4Tpc44h[XO\|YYm=		NHvaZYk6OCCvaX7z		NV7zOVZSUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtKGynbnf0bEBPNXSncn3pcoFtKEirc{[teIFo\2WmIFPLNoFteGijIHX4dJJme3OnZDDpckBU\jJzIHnud4VkfCClZXzsd{B2e2mwZzDDT\|J1cWSnIHHzJJN2[nO2cnH0[UB1emWjdHXkJIZweiB{MDDtbY5{KG2nYYP1doVlKGGodHXyJFkxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiTXfDcFIh[nliY3HsbZBmeiCvb3LpcIl1gSC\|aHnmeEBie3OjeTygTWM2OCB;IECuNFA{KM7:TT6=	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV3OUK3PEc,Ojl3NUmyO\|g9N2F-
Vero E6	NHzkSFNCdnSrdnnyZYwh[XO\|YYm=		MYK0PEBp		M1vwbGlEPTBiZn;yJIFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JHNCWlNvQ3;WMVIhcW5idHjlJHZmem9iRU[gZ4VtdCCuaX7lJIF1KDR6IHigZpkhcW2vdX7v[ox2d3Knc3PlcoNmNWKjc3XkJIF{e2G7IDjk[ZRm[3SrbnegeIhmKH[rcnHsJG5RKHC{b4TlbY4hcW5idHjlJI52[2yndYOgc4YhfGinIG\ldo8hTTZiY3XscJMqNixiSVO1NEA:KDNwOEmwOFUh\|ryPLh?=	MlrGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzJ\|NUO4OVkoRjN{M{WzPFU6RC:jPh?=
A549	NHjaRmNHfW6ldHnvckBie3OjeR?=	MV2zNEB2VQ>?	M3HFfFQ5KGi{cx?=		MknoTY5pcWKrdHnvckBw\iCFS{KtcYVlcWG2ZXSgUW1ROiCjY4TpeoF1cW:wIHnuJIh2dWGwIFG1OFkh[2WubIOgZZQhOzBidV2gZYZ1\XJiNEigbJJ{KGK7IHflcIF1cW5veontc4dz[XCqeR?=	MnuyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMUKxNlQoRjJ2MEGyNVI1RC:jPh?=
A549	M4\ldmZ2dmO2aX;uJIF{e2G7	M2PUWlExKHWP	Mn:wNVUhfG9iM{CgcYlvew>?		M3v2W2lvcGmkaYTpc44hd2ZiQ1uyMY1m\GmjdHXkJGVTUyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hSTV2OTDj[YxteyCjdDCxNEB2VSCjZoTldkAyPSC2bzCzNEBucW6\|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q>	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDBzMkGyOEc,OjRyMUKxNlQ9N2F-
A549	MVPGeY5kfGmxbjDhd5NigQ>?	Mmn0NUB1dyBzMDD1US=>	M1fv[VI1KGi{cx?=		M1f4fWlvcGmkaYTpc44hd2ZiQ1uyMY1m\GmjdHXkJG1VOS2PTWCg[ZhxemW\|c3nvckBqdiCqdX3hckBCPTR7IHPlcIx{KGG2IEGgeI8hOTBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBu\XSqb3S=	NEfuNZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECxNlEzPCd-MkSwNVIyOjR:L3G+
A549	NGTmU\|RHfW6ldHnvckBie3OjeR?=	M1\0NFExKHWP			MnHKTY5pcWKrdHnvckBw\iCFS{KtcYVlcWG2ZXSgSXJMKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBCPTR7IHPlcIx{KGG2IEGwJJVOKGK7IGfld5Rmem5iYnzveEBu\XSqb3S=	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDBzMkGyOEc,OjRyMUKxNlQ9N2F-
A549	MUfGeY5kfGmxbjDhd5NigQ>?	MofFNVAhfU1?	M1rZTVI1KGi{cx?=		NEnGSZFKdmirYnn0bY9vKG:oIFPLNk1u\WSrYYTl[EBCU1RicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEF3NEmgZ4VtdHNiYYSgNVAhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R?	NUfsdVF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNVIyOjRpPkK0NFEzOTJ2PD;hQi=>
A549	NF;reY9HfW6ldHnvckBie3OjeR?=	MmrNNVAhfU1?	NG[0d4Q1KHSxIEK0JIhzew>?		MVnJcohq[mm2aX;uJI9nKEONMj3t[YRq[XSnZDDBT3QheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGE2PDliY3XscJMh[XRiMUCgeW0h[W[2ZYKgOEB1dyB{NDDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?=	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDBzMkGyOEc,OjRyMUKxNlQ9N2F-
U-2 OS	M3HDepFJXFNiYYPzZZk>				NHHqfHhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVT2yJG9UKGOnbHzz	MmPVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
A673	NVXXemJweUiWUzDhd5NigQ>?				MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>?	NY\4dVhERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
DAOY	MUnxTHRUKGG\|c3H5				M2LpbpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy\|	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Saos-2	NH;2SolyUFSVIHHzd4F6				M3;r[5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	Mo\EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
BT-37	M4\B[5FJXFNiYYPzZZk>				M2DFWpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?=	NW\TdolKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD	MmjqdWhVWyCjc4PhfS=>				MlH2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-SH	NIK5OIZyUFSVIHHzd4F6				NVzQenVpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM>	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-12	MoXYdWhVWyCjc4PhfS=>				M4WxVpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
MG 63 (6-TG R)	NHr1fXVyUFSVIHHzd4F6				M4rqZpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?=	M1HGblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643	Mm\rdWhVWyCjc4PhfS=>				NGDLWZdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz	NGjxO\|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
OHS-50	NH\VSJdyUFSVIHHzd4F6				MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy\|	MmPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh41	M1;zU5FJXFNiYYPzZZk>				MnLxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN?	NVL2OW5DRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2	M3zafJFJXFNiYYPzZZk>				MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?=	M3HSXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	M1jrcpFJXFNiYYPzZZk>				MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
NB-EBc1	NUm2eJN3eUiWUzDhd5NigQ>?				M{\vbpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz	M3jCZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5	NWDDcHRbeUiWUzDhd5NigQ>?				Ml;6dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy\|	MlHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh18	M{O3SJFJXFNiYYPzZZk>				MnrxdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN?	M1nqeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-S6K1(T389) / S6K1 / p-S6(S235/236) / S6; PubMed: 30683840 Cell Death Dis DLD-1 cells were incubated with 25 μM silmitasertib for 16 h. The levels of the indicated proteins were analyzed by western blot. p-AKT(S129) / p-AKT(T308) / p-AKT(S473) / AKT / p-ERK / ERK / TP53 / p-p21(Th145) / p21 / Bcl-xl; PubMed: 25798061 Int J Biol Sci CX-4945 altered PI3K/AKT/Bcl-XL, ERK/AP-1 and TP53/p21proteins in HNSCC. UM-SCC-1 (left) and UM-SCC-46 (right) cell lines were treated with 4 and 10 μM CX-4945, whole cell lysates were harvested 6 and 24 hours after treatment, and subjected to SDS-PAGE and Western blot of indicated proteins. β-action was used as a loading control. p-Smad2 (Cytosol) / Smad2/3 (Cytosol) / Smad2/3 (Nucleus) / Twist / Snail; PubMed: 24023938 PLoS One The effect of CX-4945 on TGF-β1-induced activation of Smad and expression of Snail and Twist was evaluated using Western blot analysis. Briefly, after 24 h serum starvation, A549 cells were treated with TGF-β1 (5 ng/ml) alone or in combination with CX-4945 in media containing 0.1% FBS for 48 h. Cytosolic and Nuclear fractions were obtained. Actin and histone H3 were used as internal control of cytosolic and nuclear fraction, respectively. The relative, normalized ratio between p-Smad2 and actin was presented.	30683840 25798061 24023938
Immunofluorescence	β-catenin; PubMed: 24023938 PLoS One Nuclear translocation of β-catenin and its inhibition by CX-4945 were confirmed by immunocytochemistry. Nuclei were counterstained with Hoechst 33342. All scale bars represent 20 µm. E-cadherin / Vimentin; PubMed: 24023938 PLoS One The effect of CX-4945 on the TGF-β1-induced expression of epithelial and mesenchymal markers was evaluated by immunocytochemistry. Briefly, after 24 h serum starvation, A549 cells were treated with TGF-β1 (5 ng/ml) alone or in combination with CX-4945 in media containing 0.1% FBS for 72 h. All scale bars represent 200 µm.	24023938
Growth inhibition assay	Cell viability; PubMed: 30316146 Transl Oncol CX-4945 decreases cell viability of HuCCT1, EGI-1, and Liv27 CCA cell lines in dose-dependent manner (IC50of 7.3, 9.5, and 9.4 μM, respectively) (A)	30316146

体内研究

在BT-474模型中，一天两次口服25 mg/kg或75 mg/kg的CX-4945，具有强效的抗癌活性，TGI分别为88% 和97%，每组实验动物9只中有2只其肿瘤的体积大小比初期的要减少50%。在BxPC-3模型中，一天两次用75 mg/kg的CX-4945处理，TGI为93%，在治疗期结束时，有3只动物没发现还有残留的肿瘤^[1]。在PC3异种移植的模型中，用25 mg/kg, 50 mg/kg或 75 mg/kg的CX-4945处理，能抑制肿瘤生长，TGI分别为19%, 40%和86%^[2]

激酶实验：^[2]	- 合并 CK2激酶实验: 将10 μL稀释缓冲液(ADB; 20 mM MOPS, pH 7.2, 25 mM β-磷酸甘油, 5 mM EGTA, 1 mM原钒酸钠和 1 mM 二硫苏糖醇)，10 μL多肽底物(RRRDDDSDDD, 溶于ADB，浓度1mM)和10 μL重组的人源CK2(ααββ-全酶, 25 ng溶于ADB)混合，加入10 μL CX-4945。加入10μLATP溶液(90% 75 mM MgCl ₂, 75 μM ATP (终浓度15 μM)溶于ADB; 10% [γ-³³P]ATP (储存1 mCi/100 μL; 3000 Ci/mM起始反应，30 ℃反应10分钟。用100 μL的0.75%的磷酸终止反应，然后转移到磷酸纤维素滤板上过滤。每个孔用0.75%磷酸洗5次，真空抽干5分钟，再每孔加入15 μL闪烁液，然后用Wallac荧光计数器检测残留的放射性。通过对0.0001 μM 到1 μM的8个浓度的CX-4945实验结果的检测，计算出IC50。
细胞实验：^[1]	- 合并 Cell lines: SKBr3, MDA-MB-453, BT-474, ZR-75-1, MDA-MB-231, MDA-MB-468, T47D, MCF 7, Hs578T, MDA-MB-361, UACC-812, 等等 Concentrations: 溶于 DMSO, 终浓度 ~100 μM Incubation Time: 4 天 Method: 在用药处理前，在合适的培养基中按每孔3000个细胞的浓度接种细胞培养24小时，然后用不同浓度的CX-4945处理细胞。接种悬浮细胞并处理相同的天数。接着孵育4天，加入Alamar Blue (20 μL, 体积比每孔10%)，然后于37℃孵育4-5小时。检测荧光，激发光为530-560 nm，放射光为590 nm。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: 注射了BxPC-3 或BT-474细胞的免疫缺陷的雌鼠 Dosages: 25或75 mg/kg Administration: 每日两次口服 (Only for Reference)

参考文献

[4] Bliesath J, et al. Cancer Lett, 2012, 322(1), 113-118.

- 合并

溶解度 (25°C)

体外	DMSO	16 mg/mL (45.74 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 1% CMC Na	30mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Silmitasertib (CX-4945) SDF

分子量	349.77
化学式	C₁₉H₁₂ClN₃O₂
CAS号	1009820-21-6
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04668209	Recruiting	Drug: Silmitasertib	Coronavirus	University of Arizona\|Senhwa Biosciences Inc.	January 1 2021	Phase 2
NCT04663737	Active not recruiting	Drug: Silmitasertib\|Drug: SOC	Covid19	Chris Recknor MD\|Senhwa Biosciences Inc.	December 3 2020	Phase 2
NCT03904862	Recruiting	Drug: CX 4945	Medulloblastoma Childhood	Pediatric Brain Tumor Consortium\|St. Jude Children''s Research Hospital\|National Cancer Institute (NCI)	March 18 2019	Phase 1\|Phase 2
NCT02128282	Active not recruiting	Drug: CX-4945\|Drug: Cisplatin\|Drug: Gemcitabine	Cholangiocarcinoma	Senhwa Biosciences Inc.	June 2014	Phase 1\|Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
How to reconstitute the compound (S2248) for in vivo uses?
回答：
For injection, CX-4945 can be dissolved in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 5mg/ml clearly. When making the solution, please dissolve the compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm the solution in water bath at about 45-50℃. Then add PEG and Tween. After they mixed well, dilute with water. For oral gavage, CX-4945 can be dissolved in 1% CMC Na at 30mg/ml as a homogeneous suspension. This is a common formulation for oral gavage, and is convenience to prepare.

研究领域

产品类型

定制您的化合物库

Silmitasertib (CX-4945)

客户使用Selleck生产的Silmitasertib (CX-4945)发表文献91篇：

产品安全说明书

Casein Kinase抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Silmitasertib (CX-4945) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

技术支持

常见问题及建议解决方法