CB 5083

Cat. No. 7379 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent p97 ATPase inhibitor

化学名： 1-[7,8-Dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide

纯度： ≥98% (HPLC)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for CB 5083

CB 5083 is a potent p97 inhibitor, inhibiting the D2 ATPase domain (IC₅₀ = 11 nM). CB 5083 shows broad antitumor activity and inhibits tumor growth in vivo. CB 5083 is cytotoxic to A549 cancer cells (IC₅₀ = 680 nM) and reduces cell viablility in a range of colorectal cancer cell lines. Increases CHOP and GRP78 protein levels, upregulates PD-L1 mRNA levels and results in the loss of aggresomes.

技术数据 for CB 5083

分子量	413.48
公式	C₂₄H₂₃N₅O₂
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	1542705-92-9
PubChem ID	73051434
InChI Key	RDALZZCKQFLGJP-UHFFFAOYSA-N
Smiles	O=C(N)C1=CC=CC2=C1C=C(N2C=3N=C(NCC=4C=CC=CC4)C5=C(N3)CCOC5)C

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for CB 5083

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	41.35	100
	ethanol	41.35	100

制备储备液 for CB 5083

以下数据基于产品分子量 413.48。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.42 mL	12.09 mL	24.18 mL
5 mM	0.48 mL	2.42 mL	4.84 mL
10 mM	0.24 mL	1.21 mL	2.42 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

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产品说明书 for CB 5083

分析证书/产品说明书

化学品安全技术说明书

参考文献 for CB 5083

参考文献是支持产品生物活性的出版物。

Mukkavalli et al (2021) The p97-UBXN1 complex regulates aggresome formation. J.Cell Sci. 134 PMID: 33712450

Vekaria et al (2016) Targeting p97 to disrupt protein homeostasis in cancer. Front.Oncol. 6 PMID: 27536557

Vekaria et al (2019) Functional cooperativity of p97 and histone deacetylase 6 in mediating DNA repair in mantle cell lymphoma cells. Leukemia 33 1675 PMID: 30664664

Huryn et al (2019) p97: an emerging target for cancer, neurodegenerative diseases, and viral infections. J.Med.Chem. 63 1892 PMID: 31550150

Le Moigne et al (2017) The p97 inhibitor CB-5083 is a unique disrupter of protein homeostasis in models of multiple myeloma. Mol.Cancer Ther. 16 2375 PMID: 28878026

If you know of a relevant reference for CB 5083, please let us know.

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关键词: CB 5083, CB 5083 supplier, CB5083, p97, atpases, inhibitors, potent, tumor, antitumor, aggresome, valosin, containing, protein, VCP, colorectal, cancer, PD-L1, CRC, ATPase, 7379, Tocris Bioscience

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