Silmitasertib (CX-4945)
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。
Silmitasertib (CX-4945) Chemical Structure
CAS: 1009820-21-6
产品质控
批次：
纯度：
99.98%
99.98
常与Silmitasertib (CX-4945)一起在实验中被使用的化合物
Silmitasertib和Venetoclax组合可增加套细胞淋巴瘤(MCL)细胞凋亡。
Silmitasertib和Trabectedin可降低黑素瘤细胞系MM66/MP46/MP38/MM28中Bcl-2的表达，并增加Bim和Bmf的表达。
Glinkina K, et al. Invest Ophthalmol Vis Sci. 2022 Dec 1;63(13):14.
Silmitasertib和Imatinib联合抑制CK2和KIT，导致GIST882，GIST430/654和GIST48细胞中KIT/PI3K/AKT/mTOR失活。
Silmitasertib(CX-4945)和Decitabine联合使用可减少PTEN和AKT磷酸化，并抑制PI3K/AKT介导的体外和体内增殖。
Silmitasertib (CX-4945)相关产品
| 相关靶点 | CK1 CK2 | 点击展开 |
|---|---|---|
| 相关产品 | Silmitasertib (CX-4945) sodium salt D 4476 TBB IC261 (E/Z)-GO289 TTP 22 Longdaysin PF 4800567 Ellagic Acid hydrate | 点击展开 |
| 相关化合物库 | 代谢化合物库 抗癌代谢化合物库 谷氨酰胺代谢化合物库 糖代谢化合物库 脂代谢化合物库 | 点击展开 |
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| A549 | Function assay | 10 uM | 4 to 24 hrs | Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 4 to 24 hrs by Western blot method | 24012124 |
| A549 | Function assay | 10 uM | 24 hrs | Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 24 hrs by Western blot method | 24012124 |
| A549 | Function assay | 10 uM | Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM by Western blot method | 24012124 | |
| A549 | Function assay | 10 uM | 15 to 30 mins | Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM after 15 to 30 mins by Western blot method | 24012124 |
| A549 | Function assay | 30 uM | 48 hrs | Inhibition of CK2-mediated MMP2 activation in human A549 cells at 30 uM after 48 hrs by gelatin-zymography | 24012124 |
| Vero E6 | Antiviral assay | 48 h | IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells)., IC50 = 3.89045 μM. | 32353859 | |
| Sf21 | Function assay | 90 mins | Inhibition of recombinant human full length N-terminal His6-tagged CK2alpha expressed in Sf21 insect cells using CK2tide as substrate treated for 20 mins measured after 90 mins in presence of MgCl2 by caliper mobility shift assay, IC50 = 0.003 μM. | 29559278 | |
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells after 72 hrs by MTS assay, CC50 = 9.9 μM. | 26850376 | |
| Sf9 | Function assay | Inhibition of CDK2/cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate in presence of [gamma33P]ATP, IC50 = 1.8 μM. | 24681986 | ||
| K562 | Antiproliferative assay | 1 to 3 days | Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay, CC50 = 7 μM. | 23711832 | |
| U937 | Antiproliferative assay | 1 to 3 days | Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay, CC50 = 4.2 μM. | 23711832 | |
| MV4-11 | Antiproliferative assay | 1 to 3 days | Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay, CC50 = 3 μM. | 23711832 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, IC50 = 8.2 μM. | 22339433 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, IC50 = 6.5 μM. | 22339433 | |
| Hs 578T | Antiproliferative assay | 4 days | Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay, IC50 = 13.1 μM. | 21174434 | |
| MCF7 | Antiproliferative assay | 4 days | Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay, IC50 = 8.9 μM. | 21174434 | |
| MDA-MB-231 | Antiproliferative assay | 4 days | Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay, IC50 = 6.4 μM. | 21174434 | |
| LNCAP | Antiproliferative assay | 4 days | Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay, IC50 = 4.7 μM. | 21174434 | |
| BxPC3 | Antiproliferative assay | 4 days | Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay, IC50 = 4.4 μM. | 21174434 | |
| A549 | Antiproliferative assay | 4 days | Antiproliferative activity against human A549 cells after 4 days by alamar blue assay, IC50 = 3 μM. | 21174434 | |
| Jurkat | Antiproliferative assay | 4 days | Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay, IC50 = 2.5 μM. | 21174434 | |
| HCT116 | Antiproliferative assay | 4 days | Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay, IC50 = 2.2 μM. | 21174434 | |
| MIAPaCa2 | Antiproliferative assay | 4 days | Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay, IC50 = 1.1 μM. | 21174434 | |
| Jurkat | Function assay | Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay, IC50 = 0.1 μM. | 21174434 | ||
| HDMEC | Function Assay | 1 μM | 24 h | affects subcellular localization of NFATc1 and phospho-p65 | 26381437 |
| HDMEC | Function Assay | 0.25/0.5/1 μM | 24 h | reduces expression of VCAM-1 but not ICAM-1 | 26381437 |
| A549 | Function Assay | 3/10 μM | 48 h | suppresses the micropillar-induced expression of p-FAK | 26318800 |
| HDMEC | Function Assay | 50 μM | 1/5 h | decreases the nuclear signal of phosphorylated p65 in TNF-α-stimulated HDMEC | 26189586 |
| HDMEC | Kinase Assay | 1-50 μM | 5 h | decreases CK2 kinase activity without affecting cell viability | 26189586 |
| HEK293 | Function Assay | 3 μM | 5 h | CK2 phosphorylates eIF3j at Ser127 | 25887626 |
| LAMA84 | Kinase Assay | 0.5 μM | 15 min | reduces CK2 kinase activity | 25887626 |
| Hela | Kinase Assay | 0.5 μM | 15 min | reduces CK2 kinase activity | 25887626 |
| HEK293 | Kinase Assay | 0.5 μM | 15 min | reduces CK2 kinase activity | 25887626 |
| UM-SCC46 | Function Assay | 0.5/4/10 μM | 72 h | down-regulates the expression of NF-ĸB, Bcl-XL, p53, p21, AP-1 and up-regulates the expression IL-8 concentration dependently | 25798061 |
| UM-SCC1 | Function Assay | 0.5/4/10 μM | 72 h | down-regulates the expression of NF-ĸB, Bcl-XL and up-regulates the expression of p53, p21, AP-1 and IL-8 concentration dependently | 25798061 |
| UM-SCC46 | Growth Inhibition Assay | 0.1-30 μM | 1-5 d | IC50=3.4 μM | 25798061 |
| Raji | Growth Inhibition Assay | 5-25 μM | 48 h | inhibits cell growth concentration dependently | 25788269 |
| Oci Ly 19 | Growth Inhibition Assay | 5-25 μM | 48 h | inhibits cell growth concentration dependently | 25788269 |
| Oci Ly 18 | Growth Inhibition Assay | 5-25 μM | 48 h | inhibits cell growth concentration dependently | 25788269 |
| Oci Ly 1 | Growth Inhibition Assay | 5-25 μM | 48 h | inhibits cell growth concentration dependently | 25788269 |
| Oci Ly 10 | Growth Inhibition Assay | 5-25 μM | 48 h | inhibits cell growth concentration dependently | 25788269 |
| Oci Ly 3 | Growth Inhibition Assay | 5-25 μM | 48 h | inhibits cell growth concentration dependently | 25788269 |
| NU-DUL | Growth Inhibition Assay | 5-25 μM | 48 h | inhibits cell growth concentration dependently | 25788269 |
| H358 | Apoptosis Assay | 10 μM | 72 h | induces apoptosis | 25750308 |
| Calu-1 | Apoptosis Assay | 10 μM | 72 h | induces apoptosis | 25750308 |
| PC9/ER | Function Assay | 5 µM | 48 h | induces autophagy | 25486409 |
| PC9/GR | Function Assay | 5 µM | 48 h | induces autophagy | 25486409 |
| H2052 | Growth Inhibition Assay | 0.01-30 μM | 72 h | IC50=2.0 μM | 25422081 |
| UM-SCC-46 | Clonogenic Assay | 0.5-5 μM | 14 d | inhibits clonogenic survival and sphere formation | 25379016 |
| H2170 | Function Assay | 10 μM | 30 min | attenuates PI3K-Akt-mTOR signaling | 22387988 |
| A431 | Function Assay | 10 μM | 4-24 h | enhances apoptosis with | 22387988 |
| H2170 | Function Assay | 10 μM | 4-24 h | enhances apoptosis with | 22387988 |
| LNCap | Growth Inhibition Assay | 0-30 μM | 4 d | IC50=4.59 μM | 22832316 |
| A549 | Growth Inhibition Assay | 0-30 μM | 72 h | IC50=4.15 μM, inhibits cell growth concentration dependently | 23651443 |
| H1299 | Growth Inhibition Assay | 0-30 μM | 72 h | IC50=1.80 μM, inhibits cell growth concentration dependently | 23651443 |
| A549 | Function Assay | 1/10 μM | 48 h | leads to a dose-dependent decrease in Notch reporter activity | 23651443 |
| S-LAMA84 | Function Assay | 3 μM | 24 h | reduces CK2 activity | 24012109 |
| A549 | Function Assay | 10 μM | 12/24/48 h | inhibits TGF-β1-induced migration and invasion | 24023938 |
| A549 | Function Assay | 3 μM | 48 h | inhibits TGF-β1-induced activation of Smad and expression of Snail and Twist | 24023938 |
| U-266 | Growth Inhibition Assay | 0-40 μM | 48 h | IC50=19.8 µM | 24086494 |
| Jeko-1 | Growth Inhibition Assay | 0-40 μM | 48 h | IC50=2.4 µM | 24086494 |
| INA-6 | Growth Inhibition Assay | 0-40 μM | 48 h | IC50=2.42 µM | 24086494 |
| Rec-1 | Growth Inhibition Assay | 0-40 μM | 48 h | IC50=1.46 µM | 24086494 |
| CEM-R | Growth Inhibition Assay | 1-10 μM | 48 h | IC50=4 μM | 24253024 |
| Jurkat | Growth Inhibition Assay | 1-10 μM | 48 h | IC50=4.9 μM | 24253024 |
| CEM-S | Growth Inhibition Assay | 1-10 μM | 48 h | IC50=4.6 μM | 24253024 |
| MOLT-4 | Growth Inhibition Assay | 1-10 μM | 48 h | IC50=5.7 μM | 24253024 |
| PF-382 | Growth Inhibition Assay | 1-10 μM | 48 h | IC50=4.5 μM | 24253024 |
| ALL-SIL | Growth Inhibition Assay | 1-10 μM | 48 h | IC50=5.7 μM | 24253024 |
| DND-41 | Growth Inhibition Assay | 1-10 μM | 48 h | IC50=9 μM | 24253024 |
| HPB-ALL | Growth Inhibition Assay | 1-10 μM | 48 h | IC50=6.1 μM | 24253024 |
| ALL-SIL | Apoptosis Assay | 5 μM | 24/48 h | induces apoptosis | 24253024 |
| DND-41 | Apoptosis Assay | 5 μM | 24/48 h | induces apoptosis | 24253024 |
| MOLT-4 | Apoptosis Assay | 5 μM | 24/48 h | induces apoptosis | 24253024 |
| C2C12 | Function Assay | 3 μM | 12/24/48 h | inhibits the expression of osteoclast differentiation markers and Akt phosphorylation | 24293011 |
| Nalm6 | Function Assay | 10/20 μM | 24 h | results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression | 24561792 |
| SUP-B15 | Function Assay | 10/20 μM | 24 h | results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression | 24561792 |
| SUP-B15 | Apoptosis Assay | 6/10 μM | 48 h | induces apoptosis | 24561792 |
| ARPE-19 | Kinase Assay | 5/10/20 μM | 24/48 h | inhibits CK2 kinase activity at a concentration of 5 μM | 24686080 |
| ARPE-19 | Growth Inhibition Assay | 10 μM | 24-96 h | inhibits cell growth time dependently | 24686080 |
| HCT116 | Growth Inhibition Assay | 10 μM | 24-96 h | inhibits cell growth time dependently | 24686080 |
| ARPE-19 | Function Assay | 10 μM | 4 h | causes ER-stress response over the p-eIF2α branch, but does not induce CHOP | 24686080 |
| HCT116 | Function Assay | 10 μM | 4 h | causes ER-stress response over the p-eIF2α branch, but does not induce CHOP | 24686080 |
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| A549 | Function assay | 1 to 10 uM | 24 hrs | Inhibition of CK2-mediated MT1-MMP expression in human A549 cells at 1 to 10 uM after 24 hrs by Western blot method | 24012124 |
| Jurkat | Antiproliferative assay | 1 to 3 days | Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay, CC50 = 4.5 μM. | 23711832 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50 = 5.2 μM. | 22339433 | |
| K562 | Antiproliferative assay | 4 days | Antiproliferative activity against human K562 cells after 4 days by alamar blue assay, IC50 = 5.3 μM. | 21174434 | |
| A375 | Antiproliferative assay | 4 days | Antiproliferative activity against human A375 cells after 4 days by alamar blue assay, IC50 = 3.9 μM. | 21174434 | |
| H1299 | Antiproliferative assay | 4 days | Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay, IC50 = 2.4 μM. | 21174434 | |
| PC3 | Antiproliferative assay | 4 days | Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay, IC50 = 2.1 μM. | 21174434 | |
| HDMEC | Kinase Assay | 0.25/0.5/1 μM | 24 h | reduces CK2 kinase activity, vWF expression and secretion | 26381437 |
| platelets | Kinase Assay | 1/5/10 μM | 0.5 h | reduces CK2 kinase activity and platelet aggregation | 26381437 |
| UM-SCC1 | Growth Inhibition Assay | 0.1-30 μM | 1-5 d | IC50=4.1 μM | 25798061 |
| H1299 | Apoptosis Assay | 10 μM | 72 h | induces apoptosis | 25750308 |
| H358 | Growth Inhibition Assay | 1/5/10 μM | 72 h | inhibits cell growth concentration dependently | 25750308 |
| Calu-1 | Growth Inhibition Assay | 1/5/10 μM | 72 h | inhibits cell growth concentration dependently | 25750308 |
| H1299 | Growth Inhibition Assay | 1/5/10 μM | 72 h | inhibits cell growth concentration dependently | 25750308 |
| H28 | Growth Inhibition Assay | 0.01-30 μM | 72 h | IC50=7.2 μM | 25422081 |
| A431 | Function Assay | 10 μM | 30 min | attenuates PI3K-Akt-mTOR signaling | 22387988 |
| R-LAMA84 | Function Assay | 3 μM | 24 h | reduces CK2 activity | 24012109 |
| S-LAMA84 | Growth Inhibition Assay | 2.5-10 μM | 48 h | inhibits cell growth concentration dependently | 24012109 |
| R-LAMA84 | Growth Inhibition Assay | 2.5-10 μM | 48 h | inhibits cell growth concentration dependently | 24012109 |
| Nalm6 | Apoptosis Assay | 6/10 μM | 48 h | induces apoptosis | 24561792 |
| HCT116 | Apoptosis Assay | 10 μM | 24/48 h | induces apoptosis | 24686080 |
| MDA-MB-231 | Function Assay | 2/5/10 μM | 4 h | decreases the constitutive phosphorylation of both p-S529-p65 and p-S129-Akt | 25153725 |
| MDA-MB-231 | Function Assay | 2/5/10 μM | 4 h | inhibits serine 529 phosphorylation and the expression of IL-6, IL-8 | 25153725 |
| U87-MG | Growth Inhibition Assay | 1/5/10 μM | 24/48/72 h | inhibits cell growth both concentration and time dependently | 25241897 |
| UM-SCC-1 | Clonogenic Assay | 0.5-5 μM | 14 d | inhibits clonogenic survival and sphere formation | 25379016 |
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
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)。Silmitasertib可诱导自噬并促进细胞凋亡。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 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 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]。 |
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| 激酶实验 | 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 | 细胞系 | 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 | ||
| 浓度 | 溶于 DMSO, 终浓度 ~100 μM | |||
| 孵育时间 | 4 天 | |||
| 方法 | 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。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-S6K1(T389) / S6K1 / p-S6(S235/236) / S6 p-AKT(S129) / p-AKT(T308) / p-AKT(S473) / AKT / p-ERK / ERK / TP53 / p-p21(Th145) / p21 / Bcl-xl p-Smad2 (Cytosol) / Smad2/3 (Cytosol) / Smad2/3 (Nucleus) / Twist / Snail |
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30683840 | |
| Immunofluorescence | β-catenin E-cadherin / Vimentin |
|
24023938 | |
| Growth inhibition assay | Cell viability |
|
30316146 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 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] |
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| 动物实验 | 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 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05817708 | Completed | COVID-19 |
Senhwa Biosciences Inc. |
November 7 2022 | Phase 1 |
| NCT04668209 | Terminated | Coronavirus |
University of Arizona|Senhwa Biosciences Inc. |
January 21 2021 | Phase 2 |
| NCT04663737 | Completed | Covid19 |
Chris Recknor MD|Senhwa Biosciences Inc. |
December 3 2020 | Phase 2 |
| NCT03904862 | Suspended | Medulloblastoma Childhood |
Pediatric Brain Tumor Consortium|National Cancer Institute (NCI)|American Lebanese Syrian Associated Charities (ALSAC) |
July 25 2019 | Phase 1|Phase 2 |
| NCT02128282 | Completed | Cholangiocarcinoma |
Senhwa Biosciences Inc. |
June 2014 | Phase 1|Phase 2 |
化学信息&溶解度
| 分子量 | 349.77 | 分子式 | C19H12ClN3O2 |
| CAS号 | 1009820-21-6 | SDF | Download Silmitasertib (CX-4945) SDF |
| Smiles | C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 70 mg/mL ( (200.13 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
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）
mg/kg
g
μL
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
%DMSO
%
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。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，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。
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* 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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