ART558 | Polθ Inhibitor | AmBeed-信号通路专用抑制剂

ART558 {[allProObj[0].p_purity_real_show]}

货号：A1488545

ART558是一种 Polθ 抑制剂，能够特异性地干扰 Polθ 的功能。它在癌症研究和 DNA 修复机制研究中展现了良好的应用潜力。

ART558 化学结构
CAS号：2603528-97-6

ART558 3D分子结构
CAS号：2603528-97-6

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ART558 质控信息

DNA 亚型比较

产品名称	DNA synthesis ↓ ↑	helicase ↓ ↑	RdRp ↓ ↑	ribonucleotide reductase ↓ ↑	tRNA synthetase ↓ ↑	YB-1 ↓ ↑	其他靶点	纯度
Fexinidazole	✔							98%
Daptomycin	✔							98%
Blasticidin S·HCl	✔							98%
Metronidazole	✔							98%
Daunorubicin HCl	+++ DNA synthesis, Ki: 20 nM							98%
Triglycidyl isocyanurate	✔						p53	98+%
Nedaplatin	✔							99%+
Oxolinic acid	✔							98+%
Bendamustine	✔							98+%
Trifluridine	✔							98%
Robinetin	✔							99%+
Carboplatin	✔							99%
Cidofovir	✔							99%
Cisplatin	✔							99%
Cytarabine	++++ DNA synthesis, IC50: 16 nM							98%
Acelarin	++++ DNA synthesis, EC50: 0.2 nM							99%+
Oxaliplatin	✔							98%
YK-4-279		✔						99%+
ML216		+ BLM^636-1298, IC50: 0.97 μM BLM^full-length, IC50: 2.98 μM						99%+
RK-33		✔						98%
Brr2-IN-3		✔						99%+
Phen-DC3 Trifluoromethanesulfonate		✔						98%
Favipiravir			✔					99%
Suramin sodium salt			++ RdRp, IC50: 0.26 μM					99%+
Clofarabine				++ Ribonucleotide reductase, IC50: 65 nM				97%
Didox				✔				98%
(E)-3-AP				✔				99%
Halofuginone					+++ prolyl-tRNA synthetase, Ki: 18.3nM			99%+
BC-LI-0186					+++ Leucyl-tRNA synthetase, Kd: 42.1 nM Leucyl-tRNA synthetase, IC50: 46.11 nM			98%
SU056						+ YB-1, IC50: 1.73 μM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

ART558 细胞实验

Cell Line Glioblastoma cells (GBM21) Normal Human Astrocytes (NHA) DLD1 BRCA2‒/‒cells RPE1 BRCA1‒/‒cells Brca1C61G/C61G53bp1−/−cells 53bp1−/−cells Human airway basal stem cells (ABCs) HCT116 H460 T24 U2OS WT U2OS Pol q KO RPE1 TP53‒/‒BRCA1‒/‒cells DLD1 BRCA2‒/‒cells	Concentration	Treated Time	Description	References
Glioblastoma cells (GBM21)	56.5 µM	120 hours	ART558 significantly decreases glioblastoma cell viability, induces apoptosis, and is accompanied by a reduction in cell proliferation and DNA damage.	Int J Mol Sci. 2024 Aug 23;25(17):9134.
Normal Human Astrocytes (NHA)	56.5 µM	120 hours	ART558 has a much lower impact on normal human astrocytes, especially in terms of cell viability and DNA damage.	Int J Mol Sci. 2024 Aug 23;25(17):9134.
DLD1 BRCA2‒/‒cells	5 µM	24-120 hours	ART558 induced DNA damage in BRCA2-deficient cells, evidenced by increased γH2AX foci.	Nat Commun. 2021 Jun 17;12(1):3636.
RPE1 BRCA1‒/‒cells	0.5 µM	7 days	ART558 elicited synthetic lethality in BRCA1-deficient cells and showed combinatorial effects with the PARP inhibitor olaparib.	Nat Commun. 2021 Jun 17;12(1):3636.
Brca1C61G/C61G53bp1−/−cells	10 µM		Investigated the effect of ART558 on Brca1C61G/C61G53bp1−/−cells, showing that ART558 suppressed G2/M DNA synthesis, and RAD52 inhibition could not restore DNA synthesis.	Nat Commun. 2023 Nov 29;14(1):7834.
53bp1−/−cells	10 µM		Investigated the effect of ART558 on 53bp1−/−cells, showing that ART558 suppressed G2/M DNA synthesis, but RAD52 inhibition could restore DNA synthesis.	Nat Commun. 2023 Nov 29;14(1):7834.
Human airway basal stem cells (ABCs)	5 µM		To evaluate if combining ART558 with AZD7648 further improves gene insertion efficiency, results showed improved gene insertion but induced toxicity.	Mol Ther Nucleic Acids. 2024 Sep 16;35(4):102339.
HCT116	1 µM and 3 µM		ART558 does not cause any effect in the absence of IR but effectively radiosensitizes all three BRCA-proficient cell lines from 1 mmol/L concentration.	Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.
H460	1 µM and 3 µM		ART558 does not cause any effect in the absence of IR but effectively radiosensitizes all three BRCA-proficient cell lines from 1 mmol/L concentration.	Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.
T24	1 µM and 3 µM		ART558 does not cause any effect in the absence of IR but effectively radiosensitizes all three BRCA-proficient cell lines from 1 mmol/L concentration.	Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.
U2OS WT	3 µM		U2OS WT cells were significantly radiosensitized, whereas U2OS Pol q KO cells were not radiosensitized, confirming that the radiosensitizing effect of ART558 is Pol q-specific.	Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.
U2OS Pol q KO	3 µM		U2OS Pol q KO cells were not radiosensitized by ART558, further confirming that the radiosensitizing effect of ART558 is Pol q-specific.	Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.
RPE1 TP53‒/‒BRCA1‒/‒cells	0.5 μM	7 days	Evaluate ART558 sensitivity in BRCA1-deficient cells, results showed significant reduction in cell survival	Nat Commun. 2021 Jun 17;12(1):3636.
DLD1 BRCA2‒/‒cells	5 μM	5 days	Evaluate ART558 sensitivity in BRCA2-deficient cells, results showed significant reduction in cell survival	Nat Commun. 2021 Jun 17;12(1):3636.

Cell Line

Concentration

Treated Time

Description

References

Glioblastoma cells (GBM21)

56.5 µM

120 hours

ART558 significantly decreases glioblastoma cell viability, induces apoptosis, and is accompanied by a reduction in cell proliferation and DNA damage.

Int J Mol Sci. 2024 Aug 23;25(17):9134.

Normal Human Astrocytes (NHA)

56.5 µM

120 hours

ART558 has a much lower impact on normal human astrocytes, especially in terms of cell viability and DNA damage.

Int J Mol Sci. 2024 Aug 23;25(17):9134.

DLD1 BRCA2‒/‒cells

5 µM

24-120 hours

ART558 induced DNA damage in BRCA2-deficient cells, evidenced by increased γH2AX foci.

Nat Commun. 2021 Jun 17;12(1):3636.

RPE1 BRCA1‒/‒cells

0.5 µM

7 days

ART558 elicited synthetic lethality in BRCA1-deficient cells and showed combinatorial effects with the PARP inhibitor olaparib.

Nat Commun. 2021 Jun 17;12(1):3636.

Brca1C61G/C61G53bp1−/−cells

10 µM

Investigated the effect of ART558 on Brca1C61G/C61G53bp1−/−cells, showing that ART558 suppressed G2/M DNA synthesis, and RAD52 inhibition could not restore DNA synthesis.

Nat Commun. 2023 Nov 29;14(1):7834.

53bp1−/−cells

10 µM

Investigated the effect of ART558 on 53bp1−/−cells, showing that ART558 suppressed G2/M DNA synthesis, but RAD52 inhibition could restore DNA synthesis.

Nat Commun. 2023 Nov 29;14(1):7834.

Human airway basal stem cells (ABCs)

5 µM

To evaluate if combining ART558 with AZD7648 further improves gene insertion efficiency, results showed improved gene insertion but induced toxicity.

Mol Ther Nucleic Acids. 2024 Sep 16;35(4):102339.

HCT116

1 µM and 3 µM

ART558 does not cause any effect in the absence of IR but effectively radiosensitizes all three BRCA-proficient cell lines from 1 mmol/L concentration.

Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.

H460

1 µM and 3 µM

ART558 does not cause any effect in the absence of IR but effectively radiosensitizes all three BRCA-proficient cell lines from 1 mmol/L concentration.

Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.

T24

1 µM and 3 µM

ART558 does not cause any effect in the absence of IR but effectively radiosensitizes all three BRCA-proficient cell lines from 1 mmol/L concentration.

Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.

U2OS WT

3 µM

U2OS WT cells were significantly radiosensitized, whereas U2OS Pol q KO cells were not radiosensitized, confirming that the radiosensitizing effect of ART558 is Pol q-specific.

Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.

U2OS Pol q KO

3 µM

U2OS Pol q KO cells were not radiosensitized by ART558, further confirming that the radiosensitizing effect of ART558 is Pol q-specific.

Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.

RPE1 TP53‒/‒BRCA1‒/‒cells

0.5 μM

7 days

Evaluate ART558 sensitivity in BRCA1-deficient cells, results showed significant reduction in cell survival

Nat Commun. 2021 Jun 17;12(1):3636.

DLD1 BRCA2‒/‒cells

5 μM

5 days

Evaluate ART558 sensitivity in BRCA2-deficient cells, results showed significant reduction in cell survival

Nat Commun. 2021 Jun 17;12(1):3636.

ART558 动物实验

Species Rats Nu/Nu mice	Animal Model MDA-MB-436 BRCA1 mutant SHLD2‒/‒xenografts HCT116 subcutaneous xenograft model	Administration	Dosage	Frequency	Description	References
Rats	MDA-MB-436 BRCA1 mutant SHLD2‒/‒xenografts		100 mg/kg	Daily administration for 76 days	ART812 significantly inhibited tumor growth and was well-tolerated.	Nat Commun. 2021 Jun 17;12(1):3636.
Nu/Nu mice	HCT116 subcutaneous xenograft model	Oral	150 mg/kg	Twice daily for 12 days	The combination of ART899 with fractionated radiation (10×2 Gy) significantly improved tumor growth delay and was well tolerated.	Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.

Species

Rats Nu/Nu mice

Animal Model

MDA-MB-436 BRCA1 mutant SHLD2‒/‒xenografts HCT116 subcutaneous xenograft model

Administration

Dosage

Frequency

Description

References

Rats

MDA-MB-436 BRCA1 mutant SHLD2‒/‒xenografts

100 mg/kg

Daily administration for 76 days

ART812 significantly inhibited tumor growth and was well-tolerated.

Nat Commun. 2021 Jun 17;12(1):3636.

Nu/Nu mice

HCT116 subcutaneous xenograft model

Oral

150 mg/kg

Twice daily for 12 days

The combination of ART899 with fractionated radiation (10×2 Gy) significantly improved tumor growth delay and was well tolerated.

Clin Cancer Res. 2023 Apr 14;29(8):1631-1642.

ART558 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.20mL

23.90mL

4.78mL

2.39mL

ART558 技术信息

CAS号	2603528-97-6
分子式	C₂₁H₂₁F₃N₄O₂
分子量	418.41
SMILES Code	O=C([C@H]1N(C2=NC(C)=CC(C(F)(F)F)=C2C#N)CC[C@H]1O)N(C)C3=CC=CC(C)=C3
MDL No.	N/A

别名
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 165 mg/mL(394.35 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

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ART558 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ART558 质控信息

ART558 细胞实验

ART558 动物实验

ART558 实验方案

ART558 技术信息

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