Silmitasertib (Synonyms: CX-4945)

目錄號: HY-50855 純度: 99.94%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計算器

Silmitasertib (CX-4945) 是一種有效、可口服、高度選擇性的 CK2 抑制劑，對 CK2α 和 CK2α' 的 IC₅₀值均為 1 nM。

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Silmitasertib Chemical Structure

CAS No. : 1009820-21-6

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可免費申領三個不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥1250	In-stock
2 mg	￥650	In-stock
5 mg	￥1000	In-stock
10 mg	￥1600	In-stock
50 mg	￥5100	In-stock
100 mg	現(xiàn)貨	詢價
200 mg		詢價
500 mg		詢價

or 大包裝詢價

* Please select Quantity before adding items.

Customer Review

Other Forms of Silmitasertib:

Silmitasertib sodium salt In-stock

MCE 顧客使用本產(chǎn)品發(fā)表的 40 篇科研文獻

•Signal Transduct Target Ther. 2023 May 10;8(1):183. [Abstract]
•Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
•Cell Stem Cell. 2023 Apr 6;30(4):450-459.e9. [Abstract]
•Nat Cell Biol. 2021 Mar;23(3):257-267. [Abstract]
•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
•Nat Commun. 2024 Oct 16;15(1):8912. [Abstract]

•Autophagy. 2024 Aug 22. [Abstract]
•Nat Commun. 2023 Feb 9;14(1):731. [Abstract]
•EMBO Mol Med. 2020 Aug 7;12(8):e11987. [Abstract]
•Cell Death Dis. 2024 Mar 16. [Abstract]
•Cell Mol Biol Lett. 2023 Oct 24;28(1):85. [Abstract]
•Biomed Pharmacother. 2024 Jul 29:178:117191. [Abstract]
•Cell Death Discov. 2024 Apr 22;10(1):185. [Abstract]
•Cell Rep. 2023 Apr 3;42(4):112339. [Abstract]
•J Med Chem. 2023 Mar 8. [Abstract]
•J Med Chem. 2023 Mar 6. [Abstract]
•Oncogene. 2022 Jan;41(4):571-585. [Abstract]
•Oncogene. 2017 Aug 24;36(34):4943-4950. [Abstract]
•Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
•J Immunol. 2023 Mar 27;ji2200598. [Abstract]
•Invest Ophthalmol Vis Sci. 2022 Dec 1;63(13):14. [Abstract]
•Cancers (Basel). 2021, 13(5), 1127.
•Cells. 2021 Jan 18;10(1):E181. [Abstract]
•Int J Mol Sci. 2021 Jan 15;22(2):E819. [Abstract]
•Int J Mol Sci. 2020 Mar 3;21(5):1718. [Abstract]
•Oncol Rep. 2017 Feb;37(2):1141-1147. [Abstract]
•J Biol Chem. 2024 Sep 30:107848. [Abstract]
•Heliyon. 2024 Aug 18;10(16):e36205. [Abstract]
•Drug Res (Stuttg). 2024 Mar 20. [Abstract]
•Biochem Biophys Res Commun. 2020 Oct 20;531(3):409-415. [Abstract]
•bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
•bioRxiv. 2024 Jul 25:2024.07.25.605073. [Abstract]
•Research Square Preprint. 2023 Oct 27.
•bioRxiv. 2023 Oct 23.
•Electronic Theses and Dissertations. 2023 Jul.
•Research Square Preprint. 2023 May 26.
•University of Concepcion. 2023.
•University of California. 2023 Feb.
•Patent. US20180263995A1.
•Oncotarget. 2016 Aug 16;7(33):53191-53203. [Abstract]

: Silmitasertib purchased from MCE. Usage Cited in: Oncol Rep. 2017 Feb;37(2):1141-1147. [Abstract]; CX-4945 increases the expression of apoptosis markers. Western blot analysis reveals that CX-4945 treatment increases the expression of cleaved PARP or cleaved caspase-3. CX-4945 treatment decreases the expression of Bcl-2 or Bcl-xL. The experiment is performed in triplicate, producing similar results.

: Silmitasertib purchased from MCE. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53191-53203. [Abstract]; MPNST cell lines show a decrease in CK2 activity in response to escalating CX-4945 concentrations (24 h) as measured by a western blot analysis using anti-CK2 substrate, and to undergo apoptosis as indicated by increased cleaved PARP.

Silmitasertib 相關產(chǎn)品

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查看所有亞型

CK1 CK2

生物活性
實驗參考方法
純度 & 產(chǎn)品資料
參考文獻

生物活性

Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC₅₀ values of 1 nM against CK2α and CK2α'.

IC₅₀ & Target^[1]

CK2α

1 nM (IC₅₀)

CK2α'

1 nM (IC₅₀)

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	IC₅₀	1 μM Compound: CX-4945	Inhibition of CK2 in human 786-0 cells assessed as decrease in Akt1 phosphorylation at Ser129 after 24 hrs by Western blot analysis Inhibition of CK2 in human 786-0 cells assessed as decrease in Akt1 phosphorylation at Ser129 after 24 hrs by Western blot analysis	[PMID: 30689946]
786-0	EC₅₀	1 μM Compound: CX-4945	Inhibition of CK2 in human 786-0 cells assessed as decrease in alpha-catenin phosphorylation at Ser641 after 24 hrs by Western blot analysis Inhibition of CK2 in human 786-0 cells assessed as decrease in alpha-catenin phosphorylation at Ser641 after 24 hrs by Western blot analysis	[PMID: 30689946]
786-0	EC₅₀	5.3 μM Compound: CX-4945	Inhibition of CK2 in human 786-0 cells assessed as reduction in STAT3 phosphorylation at Y705 after 24 hrs by Western blot analysis Inhibition of CK2 in human 786-0 cells assessed as reduction in STAT3 phosphorylation at Y705 after 24 hrs by Western blot analysis	[PMID: 30689946]
A-375	IC₅₀	3.9 μM Compound: 25n	Antiproliferative activity against human A375 cells after 4 days by alamar blue assay Antiproliferative activity against human A375 cells after 4 days by alamar blue assay	[PMID: 21174434]
A549	IC₅₀	11.6 μM Compound: CX-4945	Antiproliferative activity against human A549 cells incubated for 96 hrs by resazurin assay Antiproliferative activity against human A549 cells incubated for 96 hrs by resazurin assay	[PMID: 32435375]
A549	IC₅₀	3 μM Compound: 25n	Antiproliferative activity against human A549 cells after 4 days by alamar blue assay Antiproliferative activity against human A549 cells after 4 days by alamar blue assay	[PMID: 21174434]
A549	IC₅₀	8.2 μM Compound: 31, CX-4945	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay Antiproliferative activity against human A549 cells after 72 hrs by MTS assay	[PMID: 22339433]
A549	CC₅₀	9.9 μM Compound: CX-4945	Cytotoxicity against human A549 cells after 72 hrs by MTS assay Cytotoxicity against human A549 cells after 72 hrs by MTS assay	[PMID: 26850376]
BXPC-3	IC₅₀	4.4 μM Compound: 25n	Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay	[PMID: 21174434]
HCT-116	IC₅₀	13.21 μM Compound: CX-4945	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
HCT-116	IC₅₀	2.2 μM Compound: 25n	Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay	[PMID: 21174434]
HCT-116	GI₅₀	4.8 μM Compound: CX4945	Growth inhibition of human HCT116 cells measured after 72 hrs by sulforhodamine B assay Growth inhibition of human HCT116 cells measured after 72 hrs by sulforhodamine B assay	[PMID: 36426237]
HCT-116	IC₅₀	5.2 μM Compound: 31, CX-4945	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay	[PMID: 22339433]
HeLa	EC₅₀	2.1 μM Compound: CX-4945	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-based cytotoxicity assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-based cytotoxicity assay	[PMID: 34323071]
Hs-578T	IC₅₀	13.1 μM Compound: 25n	Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay	[PMID: 21174434]
HT-22	IC₅₀	21.3 μM Compound: 9; CX-4945	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
HT-29	IC₅₀	16 μM Compound: CX-4945	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
Jurkat	IC₅₀	0.1 μM Compound: 25n	Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay	[PMID: 21174434]
Jurkat	IC₅₀	2.5 μM Compound: 25n	Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay	[PMID: 21174434]
Jurkat	CC₅₀	4.5 μM Compound: CX-4945	Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay	[PMID: 23711832]
K562	IC₅₀	5.3 μM Compound: 25n	Antiproliferative activity against human K562 cells after 4 days by alamar blue assay Antiproliferative activity against human K562 cells after 4 days by alamar blue assay	[PMID: 21174434]
K562	CC₅₀	7 μM Compound: CX-4945	Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay	[PMID: 23711832]
L02	IC₅₀	22.98 μM Compound: CX-4945	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
LNCaP	IC₅₀	4.59 μM Compound: CX4945	Cytotoxicity against human LNCAP cells assessed as cell viability after 4 days by CCK8 method Cytotoxicity against human LNCAP cells assessed as cell viability after 4 days by CCK8 method	[PMID: 22832316]
LNCaP	IC₅₀	4.7 μM Compound: 25n	Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay	[PMID: 21174434]
LNCaP	IC₅₀	6.52 μM Compound: CX-4945	Antiproliferative activity against human LNCAP cells incubated for 96 hrs by resazurin assay Antiproliferative activity against human LNCAP cells incubated for 96 hrs by resazurin assay	[PMID: 32435375]
MCF7	IC₅₀	15.31 μM Compound: CX-4945	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
MCF7	IC₅₀	6.5 μM Compound: 31, CX-4945	Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay	[PMID: 22339433]
MCF7	IC₅₀	8.9 μM Compound: 25n	Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay	[PMID: 21174434]
MCF7	IC₅₀	9.41 μM Compound: CX-4945	Antiproliferative activity against human MCF7 cells incubated for 96 hrs by resazurin assay Antiproliferative activity against human MCF7 cells incubated for 96 hrs by resazurin assay	[PMID: 32435375]
MDA-MB-231	IC₅₀	14.25 μM Compound: 18; CX-4945	Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay	[PMID: 34908415]
MDA-MB-231	IC₅₀	6.4 μM Compound: CX-4945	Anticancer activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 4 days by Alamar blue assay Anticancer activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 4 days by Alamar blue assay	[PMID: 37077385]
MDA-MB-231	IC₅₀	6.4 μM Compound: 25n	Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay	[PMID: 21174434]
MDA-MB-468	IC₅₀	20.92 μM Compound: 18; CX-4945	Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay	[PMID: 34908415]
MIA PaCa-2	IC₅₀	1.1 μM Compound: 25n	Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay	[PMID: 21174434]
MV4-11	CC₅₀	3 μM Compound: CX-4945	Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay	[PMID: 23711832]
NCI-H1299	IC₅₀	2.4 μM Compound: 25n	Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay	[PMID: 21174434]
PBMC	CC₅₀	50 μM Compound: CX-4945	Cytotoxicity against human PHA-activated PBMC after 1 to 3 days by MTS assay Cytotoxicity against human PHA-activated PBMC after 1 to 3 days by MTS assay	[PMID: 23711832]
PC-3	IC₅₀	10.87 μM Compound: CX-4945	Antiproliferative activity against human PC3 cells incubated for 96 hrs by resazurin assay Antiproliferative activity against human PC3 cells incubated for 96 hrs by resazurin assay	[PMID: 32435375]
PC-3	IC₅₀	12.75 μM Compound: CX-4945	Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
PC-3	IC₅₀	2.1 μM Compound: 25n	Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay	[PMID: 21174434]
Sf9	IC₅₀	1.8 μM Compound: Silmitasertib	Inhibition of CDK2/cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate in presence of [gamma33P]ATP Inhibition of CDK2/cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate in presence of [gamma33P]ATP	[PMID: 24681986]
T-24	IC₅₀	12.92 μM Compound: CX-4945	Cytotoxicity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human T24 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33834781]
U-937	CC₅₀	4.2 μM Compound: CX-4945	Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay	[PMID: 23711832]

體外研究
(In Vitro)

Silmitasertib (CX-4945) 可使癌細胞相較于正常細胞發(fā)生細胞周期阻滯并選擇性誘導其凋亡，減弱 PI3K/Akt 信號傳導，并且 Silmitasertib (CX-4945) 的抗增殖活性與 CK2α 催化亞基的表達水平相關，同時減弱 PI3K/Akt 信號傳導^[1]。Silmitasertib (CX-4945) 與 PS-341 聯(lián)合使用可防止白血病細胞參與功能性未折疊蛋白反應 (UPR)，以緩沖 PS-341 介導的內(nèi)質(zhì)網(wǎng)腔蛋白毒性應激，并降低促存活內(nèi)質(zhì)網(wǎng)伴侶 BIP/Grp78 表達^[2]。
Silmitasertib (CX-4945) 通過下調(diào) CK2 表達并抑制 CK2 介導的 PI3K/Akt/mTOR 信號通路的激活，誘導血液腫瘤的細胞毒性和凋亡，并發(fā)揮抗增殖作用^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內(nèi)研究
(In Vivo)

Silmitasertib (CX-4945) (25 or 75 mg/kg, p.o.) 耐受性良好，并在小鼠異種移植模型中表現(xiàn)出強大的抗腫瘤活性，同時伴隨基于作用機制的生物標志物磷酸化 p21 (T145) 的減少^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

349.77

Formula

C₁₉H₁₂ClN₃O₂

CAS 號

1009820-21-6

性狀

固體

顏色

Yellow to orange

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : ≥ 35 mg/mL (100.07 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

0.1 M NaOH 中的溶解度 : 33.33 mg/mL (95.29 mM; ultrasonic and adjust pH to 9 with NaOH)

* "≥" means soluble, but saturation unknown.

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.8590 mL	14.2951 mL	28.5902 mL
5 mM	0.5718 mL	2.8590 mL	5.7180 mL
10 mM	0.2859 mL	1.4295 mL	2.8590 mL

查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

摩爾計算器
稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (5.95 mM); 懸濁液; 超聲助溶

此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.95 mM); 懸濁液; 超聲助溶

此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

方案一

請依序添加每種溶劑： 0.5% CMC-Na/0.5% Tween-80 in Saline water
Solubility: 9.95 mg/mL (28.45 mM); 懸濁液; 超聲助溶

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購。，Tween 80，均可在 MCE 網(wǎng)站選購。

計算結果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯(lián)系。

動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.94%

選擇批次：

Data Sheet (647 KB) SDS (393 KB)

COA (191 KB) LCMS (98 KB) 元素分析報告 (208 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻

[1]. Siddiqui-Jain A, et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 2010 Dec 15;70(24):10288-98. [Content Brief]

[2]. Buontempo F, et al. Synergistic cytotoxic effects of PS-341 and CK2 inhibitor CX-4945 in acute lymphoblastic leukemia: turning off the prosurvival ER chaperone BIP/Grp78 and turning on the pro-apoptotic NF-κB. Oncotarget. 2016 Jan 12;7(2):1323-40. [Content Brief]

[3]. Chon HJ, et al. The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies. Front Pharmacol. 2015 Mar 31;6:70. [Content Brief]

Cell Assay ^[1]	Various cell lines are seeded at a density of 3,000 cells per well 24 hours prior to treatment, in appropriate media, and then treated with indicated concentrations of Silmitasertib (CX-4945). Suspensions cells are seeded and treated on the same day. Following 4 days of incubation, Alamar Blue (20 μL, 10% of volume per well) is added and the cells are further incubated at 37°C for 4-5 hours. Fluorescence with excitation wavelength at 530-560 nm and emission wavelength at 590 nm is measured. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Xenografts are initiated by subcutaneous injection of BxPC-3 cells into the right hind flank region of each mouse or BT-474 cells are injected into the mammary fat pad of mice implanted with estrogen pellets. When tumors reach a designated volume of 150-200 mm³, animals are randomized and divided into groups of 9 to 10 mice per group. Silmitasertib (CX-4945) is administered by oral gavage twice daily at 25 or 75 mg/kg for 31 and 35 consecutive days for the BT-474 and BxPC-3 models, respectively. Tumor volumes and body weights are measured twice weekly. The length and width of the tumor are measured with calipers and the volume calculated using the following formula: tumor volume=(length × width²)/2. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻	[1]. Siddiqui-Jain A, et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 2010 Dec 15;70(24):10288-98. [Content Brief] [2]. Buontempo F, et al. Synergistic cytotoxic effects of PS-341 and CK2 inhibitor CX-4945 in acute lymphoblastic leukemia: turning off the prosurvival ER chaperone BIP/Grp78 and turning on the pro-apoptotic NF-κB. Oncotarget. 2016 Jan 12;7(2):1323-40. [Content Brief] [3]. Chon HJ, et al. The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies. Front Pharmacol. 2015 Mar 31;6:70. [Content Brief]

Silmitasertib 相關分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

0.1 M NaOH / DMSO	1 mM	2.8590 mL	14.2951 mL	28.5902 mL	71.4755 mL
	5 mM	0.5718 mL	2.8590 mL	5.7180 mL	14.2951 mL
	10 mM	0.2859 mL	1.4295 mL	2.8590 mL	7.1476 mL
	15 mM	0.1906 mL	0.9530 mL	1.9060 mL	4.7650 mL
	20 mM	0.1430 mL	0.7148 mL	1.4295 mL	3.5738 mL
	25 mM	0.1144 mL	0.5718 mL	1.1436 mL	2.8590 mL
	30 mM	0.0953 mL	0.4765 mL	0.9530 mL	2.3825 mL
	40 mM	0.0715 mL	0.3574 mL	0.7148 mL	1.7869 mL
	50 mM	0.0572 mL	0.2859 mL	0.5718 mL	1.4295 mL
	60 mM	0.0477 mL	0.2383 mL	0.4765 mL	1.1913 mL
	80 mM	0.0357 mL	0.1787 mL	0.3574 mL	0.8934 mL
DMSO	100 mM	0.0286 mL	0.1430 mL	0.2859 mL	0.7148 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Silmitasertib1009820-21-6CX-4945CX4945CX 4945Casein KinaseAutophagyInhibitorinhibitorinhibit

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Silmitasertib (Synonyms: CX-4945)

Customer Review

Other Forms of Silmitasertib:

MCE 顧客使用本產(chǎn)品發(fā)表的 40 篇科研文獻

Silmitasertib 相關產(chǎn)品

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純度 & 產(chǎn)品資料

參考文獻

摩爾計算器

稀釋計算器

Silmitasertib 相關分類

完整儲備液配制表

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Silmitasertib (Synonyms: CX-4945)

Customer Review

Other Forms of Silmitasertib:

Silmitasertib 相關抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 40 篇科研文獻

Silmitasertib 相關產(chǎn)品

•相關化合物庫:

•同靶點產(chǎn)品:

•同靶點蛋白產(chǎn)品:

查看 Casein Kinase 亞型特異性產(chǎn)品:

生物活性

實驗參考方法

純度 & 產(chǎn)品資料

參考文獻

Silmitasertib 相關抗體:

摩爾計算器

稀釋計算器

Silmitasertib 相關分類

完整儲備液配制表

Keywords:

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