Silmitasertib (CX-4945)

目录号:S2248

Silmitasertib (CX-4945) Chemical Structure

Molecular Weight(MW): 349.77

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)。Phase 1/2。

规格 价格 库存 购买数量  
RMB 2381.77 现货
RMB 1418.29 现货
RMB 2604.97 现货
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客户使用该产品的6个实验数据:

  • Nat Commun 2014 5, 3393. Silmitasertib (CX-4945) purchased from Selleck.

    (E) Pretreatment with CX4945 blocks TNF-induced phosphorylation of BRMS1. H157 cells were pretreated with CX4945 (30 µM) for 2 h, followed by stimulation with TNF (20 ng/mL) for an additional 1 h. Immunofluorescence assays were performed using antibodies against BRMS1 (pS30) (red)/CK2α' (green)/DAPI (blue).

    Cancer Res, 2016, 76(9):2675-86. Silmitasertib (CX-4945) purchased from Selleck.

  • Immunofluorescence analysis for Ser536 p-NF-κB cellular localization of RS4;11cells treated with CX-4945 (5 μM) and bortezomib (2.5 nM) either alone or in combination. Cells were treated, collected at 22 h and reacted with an antibody to Ser536 p-NF-κB which was revealed by a Cy3-conjugated secondary antibody. DAPI was used to label nuclei.

    Oncotarget, 2015, 51: S659-S660. Silmitasertib (CX-4945) purchased from Selleck.

    Cell Signal 2014 26(7), 1567-75. Silmitasertib (CX-4945) purchased from Selleck.

  • Cell Signal 2014 26(7), 1567-75. Silmitasertib (CX-4945) purchased from Selleck.

    (B and C) Jurkat cells were pretreated for 2 h with DES (3 μM) and CX-4945 (10 μM) individually or in combination, and were then treated with PMA (50 ng/mL) plus PHA (1 μg/mL) for 6 and 24 h. IL-2 mRNA expression was detected by qRT-PCR analysis (B) and the amounts of secreted IL-2 in the culture medium were measured by ELISA (C). #p < .01 (vs. the PMA/PHA, DES, and CX-4945 untreated cell population); *p < .01; **p < .001 (vs. the cell population treated with only PMA/PHA).

    Biomed Pharmacother, 2018, 98:357-363. Silmitasertib (CX-4945) purchased from Selleck.

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 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)。Phase 1/2。
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
platelets M3f3VWtqdmG|ZTDBd5NigQ>? MoH1NU82NzFyIN88US=> MkjJNE42KGh? MlXESG1UVw>? NUi3fIJuemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6KGGwZDDwcIF1\WyndDDh[4dz\WejdHnvci=> MnPCNlY{QDF2M{e=
HDMEC M1rQW2tqdmG|ZTDBd5NigQ>? M1PHcFAvOjVxMD61M|Eh|ryP MlLMNlQhcA>? M{\OfGROW09? M1q3R5Jm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUwhfleIIHX4dJJme3Orb36gZY5lKHOnY4LleIlwdg>? NFvyb28zPjN6MUSzOy=>
HDMEC MYDGeY5kfGmxbjDBd5NigQ>? NHfVdXgxNjJ3L{CuOU8yKM7:TR?= Mlu1NlQhcA>? MmTQSG1UVw>? M{fNcpJm\HWlZYOg[ZhxemW|c3nvckBw\iCYQ1HNMVEh[nW2IH7veEBKS0GPLUG= NF\ZRlUzPjN6MUSzOy=>
HDMEC MojySpVv[3Srb36gRZN{[Xl? Ml7aNUDPxE1? NWLyNmtsOjRiaB?= M1fEemROW09? NFPTZ4li\m[nY4TzJJN2[mOnbHz1cIFzKGyxY3HsbZpifGmxbjDv[kBPTkGWY{GgZY5lKHCqb4PwbI8ueDZ3 MlXKNlY{QDF2M{e=
A549  NV;NdWJoTnWwY4Tpc44hSXO|YYm= M3PzfVMwOTEEoN88US=> NXzIem1YPDhiaB?= NUPQSmhke3WycILld5NmeyC2aHWgcYlkem:yaXzsZZIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIICtSmFM MViyOlMyQDhyMB?=
HDMEC M4T1O2tqdmG|ZTDBd5NigQ>? NHXPN3AyNTVyIN88US=> MmHtOUBp M2TRc2ROW09? MoHJ[IVkemWjc3XzJGNMOiCtaX7hd4Uh[WO2aY\peJkhf2m2aH;1eEBi\m[nY4Tpcoch[2WubDD2bYFjcWyrdIm= MnzoNlYyQDl3OE[=
HDMEC MWfGeY5kfGmxbjDBd5NigQ>? MXq1NEDPxE1? NVH6Z4RGOS93IHi= NVX1dnJOTE2VTx?= NFXMSXJl\WO{ZXHz[ZMhfGinIH71Z4xm[XJic3nncoFtKG:oIIDoc5NxcG:{eXzheIVlKHB4NTDpckBVVkZvzsGtd5RqdXWuYYTl[EBJTE2HQ9Mg M4TQVFI3OTh7NUi2
HEK293 MX\LbY5ie2ViQYPzZZk> MWGwMlXDqM7:TR?= M{nuOFE2KG2rbh?= MYnEUXNQ MkX1doVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 NU\Kb2E2OjV6OEe2NlY>
Hela NEHpcFZMcW6jc3WgRZN{[Xl? Mm\sNE42yqEQvF2= M372NVE2KG2rbh?= MkPPSG1UVw>? NVPXZ5pvemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 NGX2WYwzPTh6N{[yOi=>
LAMA84 NIP2dHFMcW6jc3WgRZN{[Xl? MoP3NE42yqEQvF2= M1;oXVE2KG2rbh?= NHPSUYNFVVOR MlG5doVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 MViyOVg5PzZ{Nh?=
HEK293 MWfGeY5kfGmxbjDBd5NigQ>? M2Hh[VMh|ryP NVv3bFh{PSCq Mnr0SG1UVw>? M37uUmNMOiCyaH;zdIhwenmuYYTld{BmUUZ|ajDheEBU\XJzMke= NEP5R4gzPTh6N{[yOi=>
UM-SCC1 NXHUdZY4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37wfVAvOS1|MDFOwG0> Mnq0NU02KGR? MmDkTWM2OD12LkGg{txO NHPKN2szPTd7OEC2NS=>
UM-SCC46 MoHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDjNE4yNTNyIN88US=> NVnVRlZ4OS13IHS= NETSVI5KSzVyPUOuOEDPxE1? NHXnTZEzPTd7OEC2NS=>
UM-SCC1 NVThVok1TnWwY4Tpc44hSXO|YYm= NHvXNJgxNjVxND:xNEDPxE1? MVi3NkBp MmD0[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwh[W6mIIXwMZJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBxPTNuIICyNUwhSVBvMTDhcoQhUUxvODDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NXHUcm1sOjV5OUiwOlE>
UM-SCC46 NVjxSVBzTnWwY4Tpc44hSXO|YYm= MYCwMlUwPC9zMDFOwG0> M3KyZlczKGh? MkXK[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwtKHB3MzygdFIyNCCDUD2xJIFv\CC3cD3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25iSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MlrKNlU4QThyNkG=
NU-DUL MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf2cXc2NTJ3IN88US=> M4rRblQ5KGh? Mlj0bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MkPyNlU4QDh{Nkm=
Oci Ly 3 NFSxXZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWS1MVI2KM7:TR?= NEPB[oY1QCCq MlvxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MlO1NlU4QDh{Nkm=
Oci Ly 10 NXXZS49wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDFeo1KPS1{NTFOwG0> M13keFQ5KGh? MXLpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NFT1OWwzPTd6OEK2PS=>
Oci Ly 1 NGeyZZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj6WJNbPS1{NTFOwG0> MVi0PEBp MlTubY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NWfMfmFtOjV5OEiyOlk>
Oci Ly 18 NHHKb5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DPOVUuOjVizszN NUKxRXpsPDhiaB?= NUTl[G1RcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? Mmr5NlU4QDh{Nkm=
Oci Ly 19  MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInzVXA2NTJ3IN88US=> Mnj0OFghcA>? NVWy[JcycW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MkXwNlU4QDh{Nkm=
Raji NV61d2lNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYO1MVI2KM7:TR?= NVvhcoJtPDhiaB?= NH;RV4JqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M13FclI2Pzh6Mk[5
H1299 NIDOS4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H0e|EwPS9zMDFOwG0> MVW3NkBp M1v1eolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MYSyOVc2ODNyOB?=
Calu-1  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXyxM|UwOTBizszN M1ntOFczKGh? NWewW45ocW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MX[yOVc2ODNyOB?=
H358 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHH1TYQyNzVxMUCg{txO MlXrO|IhcA>? MULpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NUD2UW1qOjV5NUCzNFg>
H1299 NW\YdmF4SXCxcITvd4l{KEG|c3H5 NHfnXVIyOCEQvF2= MW[3NkBp MkLYbY5lfWOnczDhdI9xfG:|aYO= M2q3d|I2PzVyM{C4
Calu-1  MlvORZBweHSxc3nzJGF{e2G7 NYPLbogzOTBizszN MYe3NkBp M{jDZYlv\HWlZYOgZZBweHSxc3nz Ml3UNlU4PTB|MEi=
H358 MXvBdI9xfG:|aYOgRZN{[Xl? NELPNWcyOCEQvF2= NI\4OYY4OiCq NWTpbmlUcW6mdXPld{BieG:ydH;zbZM> NVLoNo86OjV5NUCzNFg>
PC9/GR MYTGeY5kfGmxbjDBd5NigQ>? MnziOUDDvU1? NHnUNWM1QCCq NFTRN2RqdmS3Y3XzJIF2fG:yaHHnfS=> M4jHUFI2PDh4NEC5
PC9/ER M2PZUWZ2dmO2aX;uJGF{e2G7 Mm\1OUDDvU1? MV:0PEBp MWDpcoR2[2W|IHH1eI9xcGGpeR?= M4W3SFI2PDh4NEC5
H28 M1npbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPwbW4xNjBzLUOwJO69VQ>? MnvRO|IhcA>? M{Lv[GROW09? M1q1O2lEPTB;Nz6yJO69VQ>? NETqUlIzPTR{MkC4NS=>
H2052 M{XiWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHuZ4V1OC5yMT2zNEDPxE1? MVu3NkBp MkTqSG1UVw>? MWfJR|UxRTJwMDFOwG0> NFvpU5YzPTR{MkC4NS=>
UM-SCC-1 NFzVSpNEdG:wb3flcolkKEG|c3H5 M{nsNlAvPS13IN88US=> MVyxOEBl MoDrSG1UVw>? MmTyxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w MmPFNlU{PzlyMU[=
UM-SCC-46 NH3YSnJEdG:wb3flcolkKEG|c3H5 MUmwMlUuPSEQvF2= MmrCNVQh\A>? NUH2OIV1TE2VTx?= NVz5cogzyqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u NYTYe|EyOjV|N{mwNVY>
U87-MG MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWmxM|UwOTBizszN MYKyOE81QC95MjDo MoTQSG1UVw>? NYexXHp4cW6qaXLpeJMh[2WubDDndo94fGhiYn;0bEBkd26lZX70doF1cW:wIHHu[EB1cW2nIHTldIVv\GWwdHz5 NH\OTFEzPTJ2MUi5Oy=>
MDA-MB-231 NIDaSGdHfW6ldHnvckBCe3OjeR?= MYqyM|UwOTBizszN NVezfZRVPCCq NFPycoFl\WO{ZXHz[ZMhfGinIHPvcpN1cXS3dHn2[UBxcG:|cHjvdplt[XSrb36gc4Yh[m:2aDCgdE1UPTJ7LYC2OUBidmRicD3TNVI6NUGtdB?= M3XVb|I2OTV|N{K1
MDA-MB-231 NGKxZplHfW6ldHnvckBCe3OjeR?= NEG1V5kzNzVxMUCg{txO M3ruclQhcA>? MV\pcohq[mm2czDz[ZJqdmViNUK5JJBpd3OyaH;yfYxifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhUUxvNjygTWwuQA>? MX[yOVE2Ozd{NR?=
ARPE-19 Mm\MT4lv[XOnIFHzd4F6 MWe1M|ExNzJyIN88US=> NULH[W5JOjRxNEigbC=> MXPpcohq[mm2czDDT|Ihc2mwYYPlJIFkfGm4aYT5JIF1KGFiY3;uZ4VvfHKjdHnvckBw\iB3wrFOwG0> NGXvTZMzPDZ6NkC4NC=>
ARPE-19 M2jSZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrDPFVmOTBizszN NF;wVXkzPC17NjDo NHX3S5NFVVOR NFnQfmRqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NGqwSoIzPDZ6NkC4NC=>
HCT116  NGriN3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFW4UG0yOCEQvF2= NFLlVFkzPC17NjDo NYnLOpdKTE2VTx?= NUfmWHJ5cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? M{jkZlI1Pjh4MEiw
ARPE-19 NHS5eJpHfW6ldHnvckBCe3OjeR?= MnfyNVAh|ryP MnfHOEBp NUe5SmIzTE2VTx?= NHHNN5Jk[XW|ZYOgSXIue3S{ZYPzJJJme3CxboPlJI93\XJidHjlJJAu\UmIMt8xJIJz[W6laDygZpV1KGSxZYOgco91KGmwZIXj[UBEUE:SwrC= NFP0XHgzPDZ6NkC4NC=>
HCT116  NUfKPYxSTnWwY4Tpc44hSXO|YYm= NIXJNYkyOCEQvF2= NV\mdIJVPCCq Mo\2SG1UVw>? MX;jZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? MW[yOFY5PjB6MB?=
HCT116  MnrqRZBweHSxc3nzJGF{e2G7 MnHaNVAh|ryP M4LlOlI1NzR6IHi= M3L2eGROW09? NGHPS5pqdmS3Y3XzJIFxd3C2b4Ppdy=> NGnIXpUzPDZ6NkC4NC=>
Nalm6  MUjGeY5kfGmxbjDBd5NigQ>? M4fl[lExNzJyIN88US=> MnfDNlQhcA>? Mlv0doV{fWy2czDpckBl\WO{ZXHz[YQhWFSHTjDwbI9{eGixconsZZRqd25iYYSgeIhmKEONMjD0ZZJo\XRicnXzbYR2\SCVM{iwJIFv\CClb37jc41qfGGwdDDkc5dvemWpdXzheIlwdiCxZjDQWGVPKHC{b4TlbY4h\XiycnXzd4lwdg>? MXyyOFU3OTd7Mh?=
SUP-B15 MU\GeY5kfGmxbjDBd5NigQ>? NVP1cmdGOTBxMkCg{txO MlS0NlQhcA>? NXOwVItvemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= M3nQOlI1PTZzN{my
Nalm6  NYXBSYFiSXCxcITvd4l{KEG|c3H5 M3;RNVYwOTBizszN MVW0PEBp NIK2eIFqdmS3Y3XzJIFxd3C2b4Ppdy=> M4jtZlI1PTZzN{my
SUP-B15 NHrvXJdCeG:ydH;zbZMhSXO|YYm= MlTVOk8yOCEQvF2= NX;SRnBuPDhiaB?= MWnpcoR2[2W|IHHwc5B1d3Orcx?= NYDEU3l2OjR3NkG3PVI>
C2C12 MV;GeY5kfGmxbjDBd5NigQ>? M2TRTlMh|ryP NVXLNJlPOTJxMkSvOFghcA>? NF3YRWdqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBwe3Snb3PsZZN1KGSrZn\ldoVvfGmjdHnvckBu[XKtZYLzJIFv\CCDa4SgdIhwe3Cqb4L5cIF1cW:w NWrwWGs2OjR{OUOwNVE>
Jurkat MnXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmCyNU0yOCEQvF2= MX60PEBp NF\xTJpKSzVyPUSuPUDPxE1? M2HCNFI1OjV|MEK0
CEM-R MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPNNU0yOCEQvF2= NF;NSm01QCCq MU\JR|UxRTRizszN MlvwNlQzPTNyMkS=
CEM-S NYTmU5dXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCxMVExKM7:TR?= NGL3dI81QCCq NF;hOIRKSzVyPUSuOkDPxE1? M3HlU|I1OjV|MEK0
MOLT-4 NH\JSXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVmxMVExKM7:TR?= MXm0PEBp Mm\TTWM2OD13Lkeg{txO NYTicYRyOjR{NUOwNlQ>
PF-382 M3rI[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWizXIJ7OS1zMDFOwG0> Mnn0OFghcA>? NYPS[GNbUUN3ME20MlUh|ryP MmTjNlQzPTNyMkS=
ALL-SIL MlvGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LzRlEuOTBizszN M4PLZ|Q5KGh? M374dGlEPTB;NT63JO69VQ>? MX2yOFI2OzB{NB?=
HPB-ALL NHftfoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzkXY44OS1zMDFOwG0> M4LVd|Q5KGh? MXPJR|UxRTZwMTFOwG0> NH;nV3gzPDJ3M{CyOC=>
DND-41 NH;Zb|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjUNWEyNTFyIN88US=> NXPJRXV[PDhiaB?= MUfJR|UxRTlizszN NXj5fo9wOjR{NUOwNlQ>
ALL-SIL M3HSNGFxd3C2b4Ppd{BCe3OjeR?= MYG1JO69VQ>? M{LWSlI1NzR6IHi= Mnv2bY5lfWOnczDhdI9xfG:|aYO= M4mxbFI1OjV|MEK0
DND-41 MWXBdI9xfG:|aYOgRZN{[Xl? MYe1JO69VQ>? MXuyOE81QCCq MXXpcoR2[2W|IHHwc5B1d3Orcx?= M4O2N|I1OjV|MEK0
MOLT-4 M1TldmFxd3C2b4Ppd{BCe3OjeR?= M{jNfVUh|ryP MX2yOE81QCCq NF6yTXNqdmS3Y3XzJIFxd3C2b4Ppdy=> MonpNlQzPTNyMkS=
U-266 NIfRS2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYSwUJZNOC12MDFOwG0> MofoOFghcA>? M3\YWWlEPTB;MUmuPEDDvU4EoB?= MkXHNlQxQDZ2OUS=
INA-6 M2rTfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfDRYwxNTRyIN88US=> NWnTNmx4PDhiaB?= MkjJTWM2OD1{LkSyJOK2VQ>? NIHDSGUzPDB6NkS5OC=>
Jeko-1 NGKxS3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7idYhROC12MDFOwG0> NUS5b|lDPDhiaB?= NFLtWFBKSzVyPUKuOEDDvU4EoB?= NIT6cZUzPDB6NkS5OC=>
Rec-1 NFnudINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPtNE01OCEQvF2= NIrsbpY1QCCq M3ntNGlEPTB;MT60OkDDvU4EoB?= M2rHN|I1ODh4NEm0
A549 MkDCSpVv[3Srb36gRZN{[Xl? M37NfVExKM7:TR?= NXHKUXp{OTJxMkSvOFghcA>? NFPPUGVqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgcYloemG2aX;uJIFv\CCrbo\hd4lwdg>? MkfLNlQxOjN7M{i=
A549 NWHVTlRwTnWwY4Tpc44hSXO|YYm= NIHZbpE{KM7:TR?= MWC0PEBp MYjpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiYXP0bZZifGmxbjDv[kBUdWGmIHHu[EBmgHC{ZYPzbY9vKG:oIGPuZYltKGGwZDDUe4l{fA>? NE[2R2YzPDB{M{mzPC=>
S-LAMA84 NV;kTJVJTnWwY4Tpc44hSXO|YYm= NE\VN|I{yqEQvF2= MnH0NlQhcA>? MkP5SG1UVw>? NEfvbZhz\WS3Y3XzJGNMOiCjY4Tpeol1gQ>? NHzCWJQzPDBzMkGwPS=>
R-LAMA84 MVTGeY5kfGmxbjDBd5NigQ>? NX;BWFczO8LizszN NWXHdYEyOjRiaB?= NEnLSotFVVOR Mk[4doVlfWOnczDDT|Ih[WO2aY\peJk> NVXwZnUxOjRyMUKxNFk>
S-LAMA84 NUTle5p{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFn0emczNjVvMUCg{txO MXi0PEBp MXHEUXNQ M{LJdolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MWWyOFAyOjFyOR?=
R-LAMA84 M3TsXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnLNk42NTFyIN88US=> M3;SbFQ5KGh? NF\MdYZFVVOR NEf6c5JqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NVfmWpN6OjRyMUKxNFk>
A549 M{\1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGS5eJAxNTNyIN88US=> M2TiT|czKGh? NH;Kb45FVVOR MVLJR|UxRTRwMUWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NHG0OJMzOzZ3MUS0Ny=>
H1299 M1HEPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVqwMVMxKM7:TR?= MYC3NkBp MUHEUXNQ Mn3uTWM2OD1zLkiwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= NFPqWVMzOzZ3MUS0Ny=>
A549 NWLsVIdGTnWwY4Tpc44hSXO|YYm= MoOxNU8yOCEQvF2= NFj5e5g1QCCq M4X1d2ROW09? MoDrcIVi\HNidH:gZUBld3OnLXTldIVv\GWwdDDk[YNz\WG|ZTDpckBPd3SlaDDy[ZBwenSncjDhZ5Rqfmm2eR?= NXrCTG82OjN4NUG0OFM>
LNCap M2\tSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTEe3cxNTNyIN88US=> MoPVOEBl NEDxV4NKSzVyPUSuOVnDqM7:TR?= MmjlNlI5OzJ|MU[=
A431  MXzGeY5kfGmxbjDBd5NigQ>? NGjUZXYyOCEQvF2= NIr6cmY{OCCvaX6= MlvPZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= Mnz5NlI{QDd7OEi=
H2170  NHTTcVJHfW6ldHnvckBCe3OjeR?= NXvwbW9COTBizszN NYTpc4ZuOzBibXnu M1zqe4F1fGWwdXH0[ZMhWEl|Sz3Bb5QudVSRUjDzbYdv[Wyrbne= MX2yNlM5Pzl6OB?=
A431  NEm4XJZHfW6ldHnvckBCe3OjeR?= NXjQeFVVOTBizszN MkfxOE0zPCCq NV2ySmFN\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni Mn\LNlI{QDd7OEi=
H2170  MUjGeY5kfGmxbjDBd5NigQ>? NE\ONW8yOCEQvF2= NIPxRpU1NTJ2IHi= MWPlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? MV2yNlM5Pzl6OB?=

... Click to View More Cell Line Experimental Data

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]

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)

激酶实验:[2]
+ 展开

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]
+ 展开
  • 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]
+ 展开
  • Animal Models: 注射了BxPC-3 或BT-474细胞的免疫缺陷的雌鼠
  • Formulation: 溶于DMSO, 用PBS稀释
  • Dosages: 25或75 mg/kg
  • Administration: 每日两次口服
    (Only for Reference)

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

分子量 349.77
化学式

C19H12ClN3O2

CAS号 1009820-21-6
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

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 (g) = 浓度 (mol/L) x 体积 (L) 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、MSDS / 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

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、MSDS / 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

  • 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

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02128282 Recruiting Cholangiocarcinoma Senhwa Biosciences Inc. June 2014 Phase 1|Phase 2
NCT01199718 Unknown status Multiple Myeloma Cylene Pharmaceuticals September 2010 Phase 1
NCT00891280 Unknown status Advanced Solid Tumors|Breast Cancer|Inflammatory Breast Cancer|Castleman''s Disease|Multiple Myeloma Cylene Pharmaceuticals February 2009 Phase 1

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。

  • * 必填项

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID