Silmitasertib (CX-4945)

目录号：S2248 Purity: 99.98%

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

规格	价格	库存
10mM (1mL in DMSO)	2104.83	现货
2mg	958.23	现货
5mg	1711.71	现货
50mg	7289.1	现货
1g	30221.58	现货
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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

Venetoclax (ABT-199)

Silmitasertib和Venetoclax组合可增加套细胞淋巴瘤(MCL)细胞凋亡。

Manni S, et al. Hemasphere 6 (2022): 1164-1165.

Trabectedin

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.

Imatinib

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。

Huang M, et al. Br J Cancer. 2020 Feb;122(3):372-381.

Decitabine

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。

Richter A, et al. BMC Cancer. 2019 Mar 6;19(1):202.

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

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(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]。
激酶实验	CK2激酶实验
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。
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		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]
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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
[1] Siddiqui-Jain A, et al. Cancer Res, 2010, 70(24), 10288-10298. [2] Pierre F, et al. J Med Chem, 2011, 54(2), 635-654. [3] Siddiqui-Jain A, et al. Mol Cancer Ther, 2012, 11(4), 994-1005. [4] Bliesath J, et al. Cancer Lett, 2012, 322(1), 113-118. + 展开

参考文献

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

+ 展开

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

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

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

DMSO : 69 mg/mL ( (197.27 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 16 mg/mL ( (45.74 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

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

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	1.750mg/ml (5.00mM)	以 1 mL 工作液为例,取50μL35mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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 g 每只动物给药体积 μL 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

%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。

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.

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):