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Selleck该产品发表文献15篇:

客户使用该产品的7个实验数据:

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

    CX-4945 (5 μM) induced a time-dependent dephosphorylation of Thr308 p-Akt and Ser235/236 p-S6RP.

    Leukemia, 2014, 28(3):543-53. 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 NF2xdGFMcW6jc3WgRZN{[Xl? M3;qS|EwPS9zMDFOwG0> MVKwMlUhcA>? Mke4SG1UVw>? MX3y[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImgZY5lKHCuYYTlcIV1KGGpZ4Ll[4F1cW:w NEHLW4ozPjN6MUSzOy=>
HDMEC MnHnT4lv[XOnIFHzd4F6 NEXpcWwxNjJ3L{CuOU8yKM7:TR?= MVqyOEBp NIXPZ4FFVVOR NGTmTGNz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJktKH[ZRjDlfJBz\XO|aX;uJIFv\CC|ZXPy[ZRqd25? MmOzNlY{QDF2M{e=
HDMEC MUHGeY5kfGmxbjDBd5NigQ>? MXSwMlI2NzBwNT:xJO69VQ>? NHHleJIzPCCq NVLnOmE{TE2VTx?= M{fPS5Jm\HWlZYOg[ZhxemW|c3nvckBw\iCYQ1HNMVEh[nW2IH7veEBKS0GPLUG= M3vPWFI3OzhzNEO3
HDMEC MXjGeY5kfGmxbjDBd5NigQ>? MmO5NUDPxE1? Ml\YNlQhcA>? M{n0dGROW09? MWXh[oZm[3S|IIP1ZoNmdGy3bHHyJIxw[2GuaYrheIlwdiCxZjDOSmFV[zFiYX7kJJBpd3OyaH:tdFY2 M3LyV|I3OzhzNEO3
A549  NIrXWotHfW6ldHnvckBCe3OjeR?= NHnScIw{NzFywrFOwG0> M4HVclQ5KGh? NV[5UFRTe3WycILld5NmeyC2aHWgcYlkem:yaXzsZZIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIICtSmFM NIXsOoozPjNzOEiwNC=>
HDMEC M3ruTWtqdmG|ZTDBd5NigQ>? NEW5cZkyNTVyIN88US=> MkLqOUBp MkLwSG1UVw>? MUPk[YNz\WG|ZYOgR2szKGurbnHz[UBi[3Srdnn0fUB4cXSqb4X0JIFn\mWldHnu[{Bk\WyuII\pZYJqdGm2eR?= MU[yOlE5QTV6Nh?=
HDMEC MWXGeY5kfGmxbjDBd5NigQ>? M4jsWFUxKM7:TR?= Mm[2NU82KGh? NV[1UVIyTE2VTx?= NHLoWHNl\WO{ZXHz[ZMhfGinIH71Z4xm[XJic3nncoFtKG:oIIDoc5NxcG:{eXzheIVlKHB4NTDpckBVVkZvzsGtd5RqdXWuYYTl[EBJTE2HQ9Mg NE\wboozPjF6OUW4Oi=>
HEK293 MYXLbY5ie2ViQYPzZZk> MVuwMlXDqM7:TR?= NI[xVHQyPSCvaX6= NGjrcGNFVVOR NYDyWFI{emWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 NYS0ZW9TOjV6OEe2NlY>
Hela MUHLbY5ie2ViQYPzZZk> MXOwMlXDqM7:TR?= M{jMVVE2KG2rbh?= NXr3NHRmTE2VTx?= NW\KN|I1emWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 MYSyOVg5PzZ{Nh?=
LAMA84 M3fQ[GtqdmG|ZTDBd5NigQ>? M{PhSlAvPcLizszN NEi0V2IyPSCvaX6= NXS0bIFiTE2VTx?= MUPy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= M3\GXVI2QDh5NkK2
HEK293 MnHZSpVv[3Srb36gRZN{[Xl? M4nGd|Mh|ryP NGftPYo2KGh? Mme2SG1UVw>? M13YVGNMOiCyaH;zdIhwenmuYYTld{BmUUZ|ajDheEBU\XJzMke= NH74ZZkzPTh6N{[yOi=>
UM-SCC1 NXfR[YRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Drc|AvOS1|MDFOwG0> MlTnNU02KGR? MlTSTWM2OD12LkGg{txO NHjmVpEzPTd7OEC2NS=>
UM-SCC46 NUexUmM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{ja[|AvOS1|MDFOwG0> MWqxMVUh\A>? Mo[wTWM2OD1|LkSg{txO M{W2NFI2Pzl6ME[x
UM-SCC1 MV7GeY5kfGmxbjDBd5NigQ>? MWewMlUwPC9zMDFOwG0> M4\QTlczKGh? MXvkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEBidmRidYCtdoVofWyjdHXzJJRp\SCneIDy[ZN{cW:wIH;mJJA2OyxicEKxMEBCWC1zIHHu[EBKVC16IHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? MU[yOVc6QDB4MR?=
UM-SCC46 MYjGeY5kfGmxbjDBd5NigQ>? NILaNYIxNjVxND:xNEDPxE1? NWfDe452PzJiaB?= NVX1WWMy\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExuIIC1N{wheDJzLDDBVE0yKGGwZDD1dE1z\We3bHH0[ZMhfGinIHX4dJJme3Orb36gTWwuQCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NW\YS21qOjV5OUiwOlE>
NU-DUL NHi5[3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVmyV5plPS1{NTFOwG0> NFXabGY1QCCq NVnKOo5WcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M4\jNVI2Pzh6Mk[5
Oci Ly 3 NEDrZZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\2OHhyPS1{NTFOwG0> MWO0PEBp NYPFS3FicW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M{fFeVI2Pzh6Mk[5
Oci Ly 10 M1j2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Xt[lUuOjVizszN M1;YelQ5KGh? MnLubY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M2PJcFI2Pzh6Mk[5
Oci Ly 1 M{O1fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfmPWtmPS1{NTFOwG0> MoPEOFghcA>? NYPx[Zd3cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NFT6SXMzPTd6OEK2PS=>
Oci Ly 18 NGHaNoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHub3o2NTJ3IN88US=> NFK4Sm01QCCq NFP3e2pqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NH3abFIzPTd6OEK2PS=>
Oci Ly 19  M3nWfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXEOU0zPSEQvF2= M4PKeFQ5KGh? NFrSXGVqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MXGyOVc5QDJ4OR?=
Raji NGrIc|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfYd3RJPS1{NTFOwG0> M{\2SVQ5KGh? NWC5U5RqcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MViyOVc5QDJ4OR?=
H1299 M13sNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjxNU82NzFyIN88US=> NYjJVpFQPzJiaB?= NW\xb|lrcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M4PkcFI2PzVyM{C4
Calu-1  NYf6NGtJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;CNU82NzFyIN88US=> M1vwSVczKGh? Mo[2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> Mny4NlU4PTB|MEi=
H358 NH;qeFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDTeVgyNzVxMUCg{txO M{e0WVczKGh? MmXWbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NUPQUIVQOjV5NUCzNFg>
H1299 NFnJWI5CeG:ydH;zbZMhSXO|YYm= NEXhRVIyOCEQvF2= MWm3NkBp M3TJT4lv\HWlZYOgZZBweHSxc3nz NUnX[mdTOjV5NUCzNFg>
Calu-1  M4WzSWFxd3C2b4Ppd{BCe3OjeR?= MnvINVAh|ryP NITuS|k4OiCq M4iyV4lv\HWlZYOgZZBweHSxc3nz NHPVXFAzPTd3MEOwPC=>
H358 MojORZBweHSxc3nzJGF{e2G7 MmjZNVAh|ryP MlP6O|IhcA>? M4rzNIlv\HWlZYOgZZBweHSxc3nz NIHGXo8zPTd3MEOwPC=>
PC9/GR NGjpeYlHfW6ldHnvckBCe3OjeR?= MYK1JOK2VQ>? NI[wXGM1QCCq NHrxVWhqdmS3Y3XzJIF2fG:yaHHnfS=> NWLOTVNXOjV2OE[0NFk>
PC9/ER M3HIWmZ2dmO2aX;uJGF{e2G7 Mo\TOUDDvU1? MVe0PEBp MnnubY5lfWOnczDheZRweGijZ4m= NFu1eIQzPTR6NkSwPS=>
H28 NW\yW|RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEThPWwxNjBzLUOwJO69VQ>? MVm3NkBp M3T1TGROW09? Mk\tTWM2OD15LkKg{txO NX7ifHZ{OjV2MkKwPFE>
H2052 NVr2emZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDkeGUxNjBzLUOwJO69VQ>? MWm3NkBp MUjEUXNQ NI\lOFlKSzVyPUKuNEDPxE1? M{joWlI2PDJ{MEix
UM-SCC-1 NXTlTpNWS2yxbn;n[Y5q[yCDc4PhfS=> M3vIXlAvPS13IN88US=> MlzLNVQh\A>? NEDDPIpFVVOR NFjjcYfDqGmwaHnibZR{KGOub37v[4VvcWNic4Xyeol3[WxiYX7kJJNxcGW{ZTDmc5Ju[XSrb36= M1j3[FI2Ozd7MEG2
UM-SCC-46 NGDoN4dEdG:wb3flcolkKEG|c3H5 MlSwNE42NTVizszN NHTMWocyPCCm NIP5XHBFVVOR MmHLxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w NWO3OoxYOjV|N{mwNVY>
U87-MG MnX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrYUHA3OS93L{GwJO69VQ>? NG\DZlkzPC92OD:3NkBp NU\ER|U{TE2VTx?= NUTrc2IycW6qaXLpeJMh[2WubDDndo94fGhiYn;0bEBkd26lZX70doF1cW:wIHHu[EB1cW2nIHTldIVv\GWwdHz5 NUL4XHpqOjV{NEG4PVc>
MDA-MB-231 NIfoW4dHfW6ldHnvckBCe3OjeR?= NHzDc4UzNzVxMUCg{txO MlTEOEBp MUfk[YNz\WG|ZYOgeIhmKGOxboP0bZR2fGm4ZTDwbI9{eGixconsZZRqd25ib3[gZo91cCBicD3TOVI6NXB4NTDhcoQheC2VMUK5MWFsfA>? NFXkeYIzPTF3M{eyOS=>
MDA-MB-231 Mn\xSpVv[3Srb36gRZN{[Xl? M3LTR|IwPS9zMDFOwG0> NWPCOYU3PCCq NIHabohqdmirYnn0d{B{\XKrbnWgOVI6KHCqb4PwbI9zgWyjdHnvckBidmRidHjlJIV5eHKnc4Ppc44hd2ZiSVytOkwhUUxvOB?= MV[yOVE2Ozd{NR?=
ARPE-19 MV\LbY5ie2ViQYPzZZk> MYC1M|ExNzJyIN88US=> NVPHVm9iOjRxNEigbC=> NVXvfGc1cW6qaXLpeJMhS0t{IHvpcoF{\SCjY4Tpeol1gSCjdDDhJINwdmOnboTyZZRqd25ib3[gOeKh|ryP M{DERVI1Pjh4MEiw
ARPE-19 NXzoZYNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;RN3gyOCEQvF2= NWDvVG1JOjRvOU[gbC=> NIjZTlhFVVOR NGLPUFZqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 M1q5XVI1Pjh4MEiw
HCT116  NV;STFRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoP6NVAh|ryP NUm4e|NtOjRvOU[gbC=> M2fDS2ROW09? MlzXbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M1T1U|I1Pjh4MEiw
ARPE-19 M4TJSWZ2dmO2aX;uJGF{e2G7 MVixNEDPxE1? MlixOEBp M1;iW2ROW09? M2jsVoNifXOnczDFVk1{fHKnc4OgdoV{eG:wc3Wgc5ZmeiC2aHWgdE1mUUZ{zsGgZpJidmOqLDDieZQh\G:nczDuc5QhcW6mdXPlJGNJV1EEoB?= NEDTcW8zPDZ6NkC4NC=>
HCT116  NIPhfHVHfW6ldHnvckBCe3OjeR?= MYCxNEDPxE1? M1fTbFQhcA>? NVviUFVMTE2VTx?= NX7rOoFj[2G3c3XzJGVTNXO2cnXzd{Bz\XOyb37z[UBwfmW{IITo[UBxNWWLRkNOtUBjemGwY3isJIJ2fCCmb3XzJI5wfCCrbnT1Z4UhS0iRUNMg NYr2W5VqOjR4OE[wPFA>
HCT116  MWfBdI9xfG:|aYOgRZN{[Xl? M{LsUlExKM7:TR?= NX3DfGNQOjRxNEigbC=> NFvmdINFVVOR M3SydYlv\HWlZYOgZZBweHSxc3nz NYPV[GJ{OjR4OE[wPFA>
Nalm6  MVLGeY5kfGmxbjDBd5NigQ>? M2XKXlExNzJyIN88US=> Mor2NlQhcA>? M{PLTpJme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? MmroNlQ2PjF5OUK=
SUP-B15 NVvtVIIzTnWwY4Tpc44hSXO|YYm= M{Do[VExNzJyIN88US=> MnPwNlQhcA>? NHHrPFRz\XO3bITzJIlvKGSnY4LlZZNm\CCSVFXOJJBpd3OyaH;yfYxifGmxbjDheEB1cGViQ1uyJJRiemendDDy[ZNq\HWnIGOzPFAh[W6mIHPvcoNwdWm2YX70JIRwf26{ZXf1cIF1cW:wIH;mJHBVTU5icILveIVqdiCneIDy[ZN{cW:w MoLFNlQ2PjF5OUK=
Nalm6  NVT5Xm84SXCxcITvd4l{KEG|c3H5 MUK2M|ExKM7:TR?= M1G2SlQ5KGh? MUXpcoR2[2W|IHHwc5B1d3Orcx?= NYnqXYh7OjR3NkG3PVI>
SUP-B15 MnvhRZBweHSxc3nzJGF{e2G7 NGLZfVY3NzFyIN88US=> M3PVfVQ5KGh? MWHpcoR2[2W|IHHwc5B1d3Orcx?= NXH3S|k6OjR3NkG3PVI>
C2C12 NV70NZFNTnWwY4Tpc44hSXO|YYm= MoHrN{DPxE1? MYCxNk8zPC92ODDo NGLjU2ZqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBwe3Snb3PsZZN1KGSrZn\ldoVvfGmjdHnvckBu[XKtZYLzJIFv\CCDa4SgdIhwe3Cqb4L5cIF1cW:w MUGyOFI6OzBzMR?=
Jurkat MkXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NES2PXQyNTFyIN88US=> NGLu[3g1QCCq M2K5ZWlEPTB;ND65JO69VQ>? MU[yOFI2OzB{NB?=
CEM-R MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVmxMVExKM7:TR?= MUO0PEBp NVvBRmt2UUN3ME20JO69VQ>? NYfGN3pVOjR{NUOwNlQ>
CEM-S NH\VdZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfYUokyNTFyIN88US=> MUC0PEBp Mme0TWM2OD12Lk[g{txO MWmyOFI2OzB{NB?=
MOLT-4 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\jNJJMOS1zMDFOwG0> NX;Y[2s6PDhiaB?= NYPkVY9nUUN3ME21Mlch|ryP MmX4NlQzPTNyMkS=
PF-382 NUnXfVY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnEN20yNTFyIN88US=> NI\LW5g1QCCq NFj3SYZKSzVyPUSuOUDPxE1? NITodowzPDJ3M{CyOC=>
ALL-SIL NEDqZo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3vNFUyNTFyIN88US=> MXm0PEBp MkjHTWM2OD13Lkeg{txO NXKyToprOjR{NUOwNlQ>
HPB-ALL NWnPW2Q4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zJ[VEuOTBizszN MYO0PEBp MUTJR|UxRTZwMTFOwG0> MWeyOFI2OzB{NB?=
DND-41 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr4enpqOS1zMDFOwG0> M4PpUlQ5KGh? MWXJR|UxRTlizszN Ml\vNlQzPTNyMkS=
ALL-SIL NIjFc5dCeG:ydH;zbZMhSXO|YYm= M2qwV|Uh|ryP Ml3CNlQwPDhiaB?= M3rl[Ylv\HWlZYOgZZBweHSxc3nz MWGyOFI2OzB{NB?=
DND-41 M2HsOWFxd3C2b4Ppd{BCe3OjeR?= MmLZOUDPxE1? NFrJXGYzPC92ODDo MVzpcoR2[2W|IHHwc5B1d3Orcx?= NXzFWJBPOjR{NUOwNlQ>
MOLT-4 M4LWXmFxd3C2b4Ppd{BCe3OjeR?= MUW1JO69VQ>? NWTqXZk6OjRxNEigbC=> NYe4NFZ[cW6mdXPld{BieG:ydH;zbZM> NWr4PVRkOjR{NUOwNlQ>
U-266 NWX6W2lWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrPXJUxNTRyIN88US=> NV\RdJlsPDhiaB?= NVzaU21uUUN3ME2xPU45KML3TdMg NGLyeIozPDB6NkS5OC=>
INA-6 NWHyPWNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIP2SmwxNTRyIN88US=> M132WVQ5KGh? MXnJR|UxRTJwNEKgxtVO NVHJdpU4OjRyOE[0PVQ>
Jeko-1 NITncIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlm4NE01OCEQvF2= NIP5blE1QCCq NYO4dmozUUN3ME2yMlQhyrWPwrC= NG\lNZQzPDB6NkS5OC=>
Rec-1 NULhXYlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\P[IkxNTRyIN88US=> NYfmZ5FLPDhiaB?= MkXlTWM2OD1zLkS2JOK2VcLi NUP4[2JEOjRyOE[0PVQ>
A549 MU\GeY5kfGmxbjDBd5NigQ>? NXXTWZNiOTBizszN M1\VXFEzNzJ2L{S4JIg> MkjmbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIH3p[5JifGmxbjDhcoQhcW64YYPpc44> Mm[wNlQxOjN7M{i=
A549 Mn7KSpVv[3Srb36gRZN{[Xl? NIm3XY0{KM7:TR?= MUi0PEBp NHP6T4tqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgZYN1cX[jdHnvckBw\iCVbXHkJIFv\CCneIDy[ZN{cW:wIH;mJHNv[WmuIHHu[EBVf2m|dB?= M3jBflI1ODJ|OUO4
S-LAMA84 NGDNcJBHfW6ldHnvckBCe3OjeR?= NXHoUHVnO8LizszN MVOyOEBp NXK0Uo9sTE2VTx?= MYTy[YR2[2W|IFPLNkBi[3Srdnn0fS=> NWq2[|lrOjRyMUKxNFk>
R-LAMA84 MlPzSpVv[3Srb36gRZN{[Xl? M4LXdVPDqM7:TR?= M3zSW|I1KGh? NIm1NpJFVVOR MWfy[YR2[2W|IFPLNkBi[3Srdnn0fS=> MXKyOFAyOjFyOR?=
S-LAMA84 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXJUW03Oi53LUGwJO69VQ>? NGDRdWI1QCCq NFjSb45FVVOR NWPQNGJIcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MmjpNlQxOTJzMEm=
R-LAMA84 MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorONk42NTFyIN88US=> MYi0PEBp M2XaVGROW09? MYDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MWeyOFAyOjFyOR?=
A549 NGf0SIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn70NE0{OCEQvF2= NWHtcYtLPzJiaB?= M3G1V2ROW09? MUfJR|UxRTRwMUWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 M3r0NlI{PjVzNESz
H1299 NInrb4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrtblgxNTNyIN88US=> NWrSSo5YPzJiaB?= Ml3zSG1UVw>? NYL5N5FYUUN3ME2xMlgxKM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M{SzXFI{PjVzNESz
A549 M3riZ2Z2dmO2aX;uJGF{e2G7 MWSxM|ExKM7:TR?= MlnWOFghcA>? M3HJVGROW09? NGrmfWVt\WGmczD0c{BiKGSxc3Wt[IVx\W6mZX70JIRm[3KnYYPlJIlvKE6xdHPoJJJmeG:{dHXyJIFkfGm4aYT5 MVWyN|Y2OTR2Mx?=
LNCap MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTQbIExNTNyIN88US=> MXG0JIQ> M{HWe2lEPTB;ND61PeKh|ryP MYOyNlg{OjNzNh?=
A431  MXXGeY5kfGmxbjDBd5NigQ>? NH\vUowyOCEQvF2= NIDvd5E{OCCvaX6= Mne0ZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= MlraNlI{QDd7OEi=
H2170  M4TpcWZ2dmO2aX;uJGF{e2G7 NFzTVmYyOCEQvF2= NF7pbpY{OCCvaX6= Mk\5ZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= Mn3INlI{QDd7OEi=
A431  NHK2RZFHfW6ldHnvckBCe3OjeR?= MkiyNVAh|ryP MX60MVI1KGh? M1P3d4VvcGGwY3XzJIFxd3C2b4Ppd{B4cXSqIHXycI91cW6rYh?= MkPnNlI{QDd7OEi=
H2170  MoPqSpVv[3Srb36gRZN{[Xl? NGHnbVYyOCEQvF2= NHXYWIE1NTJ2IHi= M3zubIVvcGGwY3XzJIFxd3C2b4Ppd{B4cXSqIHXycI91cW6rYh?= NH;2bGwzOjN6N{m4PC=>

... 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
NCT02128282 Recruiting Cholangiocarcinoma Senhwa Biosciences Inc. June 2014 Phase 1|Phase 2
NCT01199718 Unknown status Multiple Myeloma Cylene Pharmaceuticals September 2010 Phase 1
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
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