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

Silmitasertib (CX-4945) Chemical Structure

CAS: 1009820-21-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2104.83 现货
2mg RMB 958.23 现货
5mg RMB 1711.71 现货
50mg RMB 7289.1 现货
1g RMB 30221.58 现货
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客户使用Selleck的Silmitasertib (CX-4945)发表文献126

产品质控

批次: 纯度: 99.98%
99.74

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

Casein Kinase抑制剂选择性比较

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
UM-SCC-1 Clonogenic Assay 0.5-5 μM 14 d  inhibits clonogenic survival and sphere formation 25379016
U87-MG Growth Inhibition Assay 1/5/10 μM 24/48/72 h inhibits cell growth both concentration and time dependently 25241897
MDA-MB-231 Function Assay 2/5/10 μM 4 h inhibits serine 529 phosphorylation and the expression of IL-6, IL-8 25153725
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
HCT116  Apoptosis Assay 10 μM 24/48 h induces apoptosis 24686080
HCT116  Function Assay 10 μM 4 h causes ER-stress response over the p-eIF2α branch, but does not induce CHOP  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  Growth Inhibition Assay 10 μM 24-96 h inhibits cell growth time dependently 24686080
ARPE-19 Growth Inhibition Assay 10 μM 24-96 h inhibits cell growth time dependently 24686080
ARPE-19 Kinase Assay 5/10/20 μM 24/48 h inhibits CK2 kinase activity at a concentration of 5 μM 24686080
SUP-B15 Apoptosis Assay 6/10 μM 48 h induces apoptosis 24561792
Nalm6  Apoptosis Assay 6/10 μM 48 h induces apoptosis 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
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
C2C12 Function Assay 3 μM 12/24/48 h inhibits the expression of osteoclast differentiation markers and Akt phosphorylation 24293011
MOLT-4 Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
DND-41 Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
ALL-SIL Apoptosis Assay 5 μM 24/48 h induces apoptosis 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 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
MOLT-4 Growth Inhibition Assay 1-10 μM 48 h IC50=5.7 μM 24253024
CEM-S Growth Inhibition Assay 1-10 μM 48 h IC50=4.6 μM 24253024
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
Rec-1 Growth Inhibition Assay 0-40 μM 48 h IC50=1.46 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
U-266 Growth Inhibition Assay 0-40 μM 48 h IC50=19.8 µM  24086494
A549 Function Assay 3 μM 48 h inhibits TGF-β1-induced activation of Smad and expression of Snail and Twist 24023938
A549 Function Assay 10 μM 12/24/48 h inhibits TGF-β1-induced migration and invasion 24023938
R-LAMA84 Growth Inhibition Assay 2.5-10 μM 48 h inhibits cell growth concentration dependently 24012109
S-LAMA84 Growth Inhibition Assay 2.5-10 μM 48 h inhibits cell growth concentration dependently 24012109
R-LAMA84 Function Assay 3 μM 24 h reduces CK2 activity 24012109
S-LAMA84 Function Assay 3 μM 24 h reduces CK2 activity 24012109
A549 Function Assay 1/10 μM 48 h leads to a dose-dependent decrease in Notch reporter activity 23651443
H1299 Growth Inhibition Assay 0-30 μM 72 h IC50=1.80 μM, inhibits cell growth concentration dependently 23651443
A549 Growth Inhibition Assay 0-30 μM 72 h IC50=4.15 μM, inhibits cell growth concentration dependently 23651443
LNCap Growth Inhibition Assay 0-30 μM 4 d IC50=4.59 μM 22832316
H2170  Function Assay 10 μM 4-24 h enhances apoptosis with erlotinib 22387988
A431  Function Assay 10 μM 4-24 h enhances apoptosis with erlotinib 22387988
H2170  Function Assay 10 μM 30 min attenuates PI3K-Akt-mTOR signaling 22387988
A431  Function Assay 10 μM 30 min attenuates PI3K-Akt-mTOR signaling 22387988
UM-SCC-46 Clonogenic Assay 0.5-5 μM 14 d  inhibits clonogenic survival and sphere formation 25379016
H28 Growth Inhibition Assay 0.01-30 μM 72 h IC50=7.2 μM 25422081
H2052 Growth Inhibition Assay 0.01-30 μM 72 h IC50=2.0 μM 25422081
PC9/GR Function Assay 5 µM 48 h induces autophagy 25486409
PC9/ER Function Assay 5 µM 48 h induces autophagy 25486409
H1299 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
H358 Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
H1299 Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
Calu-1  Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
H358 Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
NU-DUL 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
Oci Ly 10 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 18 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
Raji Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
UM-SCC1 Growth Inhibition Assay 0.1-30 μM 1-5 d IC50=4.1 μM 25798061
UM-SCC46 Growth Inhibition Assay 0.1-30 μM 1-5 d IC50=3.4 μM 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 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
HEK293 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
LAMA84 Kinase Assay 0.5 μM 15 min reduces CK2 kinase activity 25887626
HEK293 Function Assay 3 μM 5 h CK2 phosphorylates eIF3j at Ser127 25887626
HDMEC Kinase Assay 1-50 μM 5 h decreases CK2 kinase activity without affecting cell viability 26189586
HDMEC Function Assay 50 μM 1/5 h decreases the nuclear signal of phosphorylated p65 in TNF-α-stimulated HDMEC  26189586
A549  Function Assay 3/10 μM 48 h suppresses the micropillar-induced expression of p-FAK 26318800
platelets Kinase Assay 1/5/10 μM 0.5 h reduces CK2 kinase activity and platelet aggregation 26381437
HDMEC Kinase Assay 0.25/0.5/1 μM 24 h reduces CK2 kinase activity, vWF expression and secretion 26381437
HDMEC Function Assay 0.25/0.5/1 μM 24 h reduces expression of VCAM-1 but not ICAM-1 26381437
HDMEC Function Assay 1 μM 24 h affects subcellular localization of NFATc1 and phospho-p65 26381437
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
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 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
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 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 Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM by Western blot method 24012124
MIAPaCa2 Antiproliferative assay 4 days Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay, IC50 = 1.1 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
HCT116 Antiproliferative assay 4 days Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay, IC50 = 2.2 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
Jurkat Antiproliferative assay 4 days Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay, IC50 = 2.5 μM. 21174434
A549 Antiproliferative assay 4 days Antiproliferative activity against human A549 cells after 4 days by alamar blue assay, IC50 = 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
BxPC3 Antiproliferative assay 4 days Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay, IC50 = 4.4 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
K562 Antiproliferative assay 4 days Antiproliferative activity against human K562 cells after 4 days by alamar blue assay, IC50 = 5.3 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
MCF7 Antiproliferative assay 4 days Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay, IC50 = 8.9 μM. 21174434
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
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50 = 5.2 μM. 22339433
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, IC50 = 6.5 μM. 22339433
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, IC50 = 8.2 μM. 22339433
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
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
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
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
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTS assay, CC50 = 9.9 μM. 26850376
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
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
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
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
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
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
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
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
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
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 Recruiting
Medulloblastoma Childhood
Pediatric Brain Tumor Consortium|St. Jude Children''s Research Hospital|National Cancer Institute (NCI)
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)

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

摩尔浓度计算器

体内溶解度
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

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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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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