Silmitasertib (Synonyms: CX-4945)

Name: Silmitasertib
Brand: MedChemExpress
SKU: HY-50855
Rating: 5.0 (56 reviews)

製品番号: HY-50855 純度: 99.81%: Data Sheet SDS COA 取扱説明書
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Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC₅₀ values of 1 nM against CK2α and CK2α'.

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CAS 番号 : 1009820-21-6

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 105	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 105	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$96	在庫あり	Estimated Time of Arrival: December 31
10 mg	$156	在庫あり	Estimated Time of Arrival: December 31
25 mg	$260	在庫あり	Estimated Time of Arrival: December 31
50 mg	$420	在庫あり	Estimated Time of Arrival: December 31
100 mg	$660	在庫あり	Estimated Time of Arrival: December 31
500 mg	$1400	在庫あり	Estimated Time of Arrival: December 31
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カスタマーレビュー

Based on 56 publication(s) in Google Scholar

Other Forms of Silmitasertib:

Silmitasertib sodium salt 在庫あり
Silmitasertib (Standard) お問い合わせ

顧客検証

Bio/Physico-chemical Assay

Flow Cytometry

: Silmitasertib purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2021 Mar;23(3):257-267. [Abstract]; BM2-TGC cells expressing either vector or DACT1 were treated with Wnt3a +/− Silmitasertib at 5 μM for 24h.

: Silmitasertib purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 Apr 22;10(1):185. [Abstract]; CK2α kinase activity was measured after treatment with silmitasertib (20 μM, 24 h). Cell lysates were used for in vitro kinase assay to detect the intensity of phosphorylated substrate.

: Silmitasertib purchased from MedChemExpress. Usage Cited in: Cells. 2021 Jan 18;10(1):181. [Abstract]; w.t. SK-N-BE cells were treated with CX-4945 (5-10 μM, 24-48 h) at the indicated time and concentration conditions. 30 μg proteins from lysates were analyzed by WB for the HIF-1α levels. Actin was used as loading control.

: Silmitasertib purchased from MedChemExpress. Usage Cited in: Cells. 2021 Jan 18;10(1):181. [Abstract]; SK-N-BE and U2OS cells were analyzed for the extracellular lactate secreted in the culture medium in 6 h, in the absence or in the presence of the indicated concentrations of CX-4945 (5-15 μM).

: Silmitasertib purchased from MedChemExpress. Usage Cited in: Cells. 2021 Jan 18;10(1):181. [Abstract]; SK-N-BE cells glycolytic stress test profile, upon treatment with vehicle (control) or the indicated concentration of CX-4945 (2-5 ，μM) for 5 h before running the Seahorse experiment.

: Silmitasertib purchased from MedChemExpress. 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 MedChemExpress. 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.

Casein Kinase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

CK1 CK2

生物活性
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純度とドキュメンテーション
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製品説明

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)

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	1 3 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 3 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	1 3 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 3 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]
786-0	EC₅₀	1 3 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 3 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]
786-0	IC₅₀	1 3 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	IC₅₀	1 3 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	5.3 3 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 3 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]
A-375	IC₅₀	3.9 3 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]
A-375	IC₅₀	3.9 3 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	CC₅₀	9.9 3 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]
A549	IC₅₀	11.6 3 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 3 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	3 3 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	CC₅₀	9.9 3 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]
A549	IC₅₀	8.2 3 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	IC₅₀	8.2 3 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 3 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]
A549	IC₅₀	11.6 3 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	11.6 3 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]
BXPC-3	IC₅₀	4.4 3 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]
BXPC-3	IC₅₀	4.4 3 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]
A549	IC₅₀	3 3 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 3 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]
HCT-116	IC₅₀	13.21 3 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	GI₅₀	4.8 3 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	2.2 3 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	IC₅₀	2.2 3 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]
BXPC-3	IC₅₀	4.4 3 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	GI₅₀	4.8 3 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 3 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]
HCT-116	IC₅₀	13.21 3 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	5.2 3 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 3 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]
HeLa	EC₅₀	2.1 3 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 3 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]
Hs-578T	IC₅₀	13.1 3 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 3 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-22	IC₅₀	21.3 3 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 3 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]
HT-29	IC₅₀	16 3 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 3 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	CC₅₀	4.5 3 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]
Jurkat	IC₅₀	2.5 3 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	IC₅₀	2.5 3 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 3 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]
Jurkat	IC₅₀	0.1 3 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]
K562	IC₅₀	5.3 3 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 3 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]
K562	CC₅₀	7 3 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]
K562	IC₅₀	5.3 3 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]
L02	IC₅₀	22.98 3 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]
L02	IC₅₀	22.98 3 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	4.7 3 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	4.59 3 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 3 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 3 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]
LNCaP	IC₅₀	4.59 3 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	6.52 3 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	8.9 3 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	15.31 3 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 3 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	6.5 3 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	9.41 3 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]
MCF7	IC₅₀	8.9 3 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 3 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]
MCF7	IC₅₀	15.31 3 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]
MDA-MB-231	IC₅₀	14.25 3 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 3 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 3 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 3 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-231	IC₅₀	14.25 3 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 3 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 3 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]
MDA-MB-468	IC₅₀	20.92 3 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 3 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]
MIA PaCa-2	IC₅₀	1.1 3 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 3 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]
MV4-11	CC₅₀	3 3 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]
HCT-116	GI₅₀	4.8 3 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]
NCI-H1299	IC₅₀	2.4 3 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]
HCT-116	IC₅₀	13.21 3 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]
NCI-H1299	IC₅₀	2.4 3 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 3 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]
HCT-116	IC₅₀	2.2 3 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]
PBMC	CC₅₀	50 3 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]
HCT-116	IC₅₀	5.2 3 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]
PC-3	IC₅₀	10.87 3 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	2.1 3 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]
PC-3	IC₅₀	10.87 3 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 3 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 3 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]
PC-3	IC₅₀	12.75 3 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]
Sf9	IC₅₀	1.8 3 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]
Sf9	IC₅₀	1.8 3 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]
HT-22	IC₅₀	21.3 3 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]
T-24	IC₅₀	12.92 3 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]
T-24	IC₅₀	12.92 3 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]
HT-29	IC₅₀	16 3 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]
HeLa	EC₅₀	2.1 3 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]
U-937	CC₅₀	4.2 3 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]
U-937	CC₅₀	4.2 3 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]
Hs-578T	IC₅₀	13.1 3 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]
Jurkat	CC₅₀	4.5 3 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]
Jurkat	IC₅₀	0.1 3 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 3 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]
K562	CC₅₀	7 3 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]
K562	IC₅₀	5.3 3 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]
L02	IC₅₀	22.98 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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-231	IC₅₀	6.4 3 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-468	IC₅₀	20.92 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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]

体外実験

Silmitasertib (CX-4945) causes cell-cycle arrest and selectively induces apoptosis in cancer cells relative to normal cells, attenuates PI3K/Akt signalingand, and the antiproliferative activity of Silmitasertib (CX-4945) is correlated with expression levels of the CK2α catalytic subunit, Attenuation of PI3K/Akt signaling^[1]. Silmitasertib (CX-4945) with PS-341 treatment prevents leukemic cells from engaging a functional UPR in order to buffer the PS-341-mediated proteotoxic stress in ER lumen, and decreases pro-survival ER chaperon BIP/Grp78 expression^[2]. Silmitasertib (CX-4945) induces cytotoxicity and apoptosis, and exerts anti-proliferative effects in hematological tumors by downregulating CK2 expression and suppressing activation of CK2-mediated PI3K/Akt/mTOR signaling pathways^[3].

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

体内実験

Silmitasertib (CX-4945) (25 or 75 mg/kg, p.o.) is well tolerated and demonstrated robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 (T145) in murine xenograft models^[1].

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

臨床実験

分子量

349.77

分子式

C₁₉H₁₂ClN₃O₂

CAS 番号

1009820-21-6

Appearance

Solid

Color

Yellow to orange

SMILES

O=C(C1=CC=C2C3=C(C(NC4=CC=CC(Cl)=C4)=NC2=C1)C=CN=C3)O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : ≥ 35 mg/mL (100.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (5.95 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.95 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/0.5% Tween-80 in Saline water
Solubility: 9.95 mg/mL (28.45 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.92%

Select Batch:

データシート (279 KB) SDS (396 KB)

COA (246 KB) HNMR (192 KB) RP-HPLC (237 KB) LCMS (512 KB) Elemental Analysis Report (105 KB)

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験 ^[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. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Silmitasertib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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)

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Silmitasertib (Synonyms: CX-4945)

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Other Forms of Silmitasertib:

Silmitasertib 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Casein Kinase アイソフォーム固有の製品をすべて表示:

生物活性

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純度とドキュメンテーション

参考文献

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Silmitasertib 関連抗体

Molarity Calculator

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Complete Stock Solution Preparation Table

Silmitasertib Related Classifications

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