Nutlin-3a (Synonyms: Rebemadlin)

目录号: HY-10029 纯度: 99.00%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Nutlin-3a (Rebemadlin) 是 Nutlin-3 的活性对映体，是一种有效的 MDM2 抑制剂。Nutlin-3a 可抑制 MDM2-p53 相互作用，稳定 p53 蛋白，从而诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)。Nutlin-3a 有潜力用于 TP53 野生型卵巢癌的研究。

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Nutlin-3a Chemical Structure

CAS No. : 675576-98-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1407	In-stock
5 mg	￥1320	In-stock
10 mg	￥1450	In-stock
25 mg	￥2300	In-stock
50 mg	￥3500	In-stock
100 mg	￥4950	In-stock
200 mg		询价
500 mg		询价

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Customer Review

Other Forms of Nutlin-3a:

Nutlin-3b In-stock
Nutlin-3 In-stock
(Rac)-Nutlin-3 询价

MCE 顾客使用本产品发表的 47 篇科研文献

: Nutlin-3a purchased from MCE. Usage Cited in: R Soc Open Sci. 2018 Aug 29;5(8):172376. [Abstract]; HEKs are transfected with CRISPR/CAS9-gRNA for miR-143 or miR-145 for 48 h and then treated with nutlin-3a and Puromycin for another 24 h. The protein expression of NRAS and target genes in the PI3 K/ATK pathway is analysed by western blotting.

: Nutlin-3a purchased from MCE. Usage Cited in: J Mater Chem B. 2017, 5, 5816-5834.; Immunofluorescence staining of p53, caspase 3, and MDM2 proteins in HepG2 cells treated with microparticles loaded with nutlin-3a and β-CD-g-CS/pDNA 5 days after commencement of the treatment.

: Nutlin-3a purchased from MCE. Usage Cited in: Eur J Med Chem. 2016 May 23;114:328-36. [Abstract]; The effects of compounds A₁, A₇, A₉ or Nutlin-3a in HCT116 cells by immunoprecipitation analysis

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC₅₀=90 nM). Nutlin-3a inhibits MDM2-p53?interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53?wild-type ovarian carcinomas^[1]^[2].

IC₅₀ & Target

MDM2-p53^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	GI₅₀	1.6 μM Compound: 1	Growth inhibition of human A2780 cells expressing MDM2 by SRB assay Growth inhibition of human A2780 cells expressing MDM2 by SRB assay	[PMID: 21875801]
A549	IC₅₀	15 μM Compound: Nutlin-3a	Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay	[PMID: 22940704]
A549	IC₅₀	15.12 μM Compound: Nutlin-3a	Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay	[PMID: 23046248]
A549	IC₅₀	4.62 μM Compound: Nutlin-3	Cytotoxicity against human A549 cells expressing wild type p53 after 72 hrs by SRB assay Cytotoxicity against human A549 cells expressing wild type p53 after 72 hrs by SRB assay	[PMID: 23611770]
A549	IC₅₀	4.62 μM Compound: Nutlin-3	Cytotoxicity against human A549 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human A549 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 23601819]
A549	GI₅₀	47.59 μM Compound: Nutlin-3a	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 24852275]
A549	IC₅₀	9.58 μM Compound: 3	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	[PMID: 30045621]
HCT-116	IC₅₀	> 20 μM Compound: Nutlin-3a	Antiproliferative activity against p53 -/- human HCT116 cells incubated for 72 hrs by MTS assay Antiproliferative activity against p53 -/- human HCT116 cells incubated for 72 hrs by MTS assay	[PMID: 30221935]
HCT-116	IC₅₀	1 μM Compound: (4S,5R)-Nutlin-3	Induction of p53-Ser15 phosphorylation in human HCT116 cells after 24 hrs Induction of p53-Ser15 phosphorylation in human HCT116 cells after 24 hrs	[PMID: 19856920]
HCT-116	IC₅₀	1.3 μM Compound: Nutlin-3a	Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay	[PMID: 30221935]
HCT-116	IC₅₀	1.39 μM Compound: (4S,5R)-Nutlin-3	Induction of p53 in human HCT116 cells coexpressing pp53TA-luc assessed as inhibition of cell proliferation after 8 hrs by firefly/renilla luciferase reporter assay Induction of p53 in human HCT116 cells coexpressing pp53TA-luc assessed as inhibition of cell proliferation after 8 hrs by firefly/renilla luciferase reporter assay	[PMID: 19856920]
HCT-116	IC₅₀	1.5 μM Compound: 1, Nutlin-3a	Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay	[PMID: 24900694]
HCT-116	IC₅₀	1.6 μM Compound: Nutlin-3	Cytotoxicity against human HCT116 cells after 72 hrs by CellTiterGlo luciferase-based assay Cytotoxicity against human HCT116 cells after 72 hrs by CellTiterGlo luciferase-based assay	[PMID: 24139845]
HCT-116	GI₅₀	13 μM Compound: 1	Cytotoxicity against human p53 expressing HCT116 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human p53 expressing HCT116 cells after 72 hrs by sulforhodamine B assay	[PMID: 21314128]
HCT-116	IC₅₀	1366 nM Compound: Nutilin-3a; 9	Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
HCT-116	GI₅₀	2.1 μM Compound: 1	Growth inhibition of human HCT116 cells expressing MDM2 by SRB assay Growth inhibition of human HCT116 cells expressing MDM2 by SRB assay	[PMID: 21875801]
HCT-116	IC₅₀	21.5 μM Compound: Nutlin-3a	Antiproliferative activity against human p53-null HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human p53-null HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 27101893]
HCT-116	GI₅₀	25.6 μM Compound: 1	Growth inhibition of p53 deficient human HCT116 cells expressing MDM2 by SRB assay Growth inhibition of p53 deficient human HCT116 cells expressing MDM2 by SRB assay	[PMID: 21875801]
HCT-116	GI₅₀	27 μM Compound: Nutlin-3a	Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay	[PMID: 29089230]
HCT-116	GI₅₀	29 μM Compound: Nutlin-3a	Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis	[PMID: 29691156]
HCT-116	GI₅₀	32.11 μM Compound: Nutlin-3a	Antiproliferative activity against human HCT116 cells expressing wild type p53 after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells expressing wild type p53 after 48 hrs by MTT assay	[PMID: 24852275]
HCT-116	GI₅₀	34 μM Compound: 1	Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by sulforhodamine B assay	[PMID: 21314128]
HCT-116	GI₅₀	39.65 μM Compound: Nutlin-3	Antiproliferative activity against human HCT116 cells expressing p53 after 24 hrs by MTS assay Antiproliferative activity against human HCT116 cells expressing p53 after 24 hrs by MTS assay	[PMID: 24268795]
HCT-116	GI₅₀	4 μM Compound: Nutlin-3a	Antiproliferative activity against human p53 +/+ HCT116 cells measured after 72 hrs by MTS assay Antiproliferative activity against human p53 +/+ HCT116 cells measured after 72 hrs by MTS assay	10.1039/C5MD00450K
HCT-116	IC₅₀	4 μM Compound: Nutlin-3a	Antiproliferative activity in p53 (+/+) human HCT116 cells incubated for 72 hrs by MTS assay Antiproliferative activity in p53 (+/+) human HCT116 cells incubated for 72 hrs by MTS assay	[PMID: 28987608]
HCT-116	GI₅₀	47.8 μM Compound: Nutlin-3a	Antiproliferative activity against human p53 -/- HCT116 cells measured after 72 hrs by MTS assay Antiproliferative activity against human p53 -/- HCT116 cells measured after 72 hrs by MTS assay	10.1039/C5MD00450K
HCT-116	IC₅₀	47.8 μM Compound: Nutlin-3a	Antiproliferative activity in p53 (-/-) human HCT116 cells incubated for 72 hrs by MTS assay Antiproliferative activity in p53 (-/-) human HCT116 cells incubated for 72 hrs by MTS assay	[PMID: 28987608]
HCT-116	IC₅₀	5.21 μM Compound: Nutlin-3a	Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 27101893]
HCT-116	GI₅₀	52.34 μM Compound: Nutlin-3	Antiproliferative activity against p53-deficient human HCT116 cells after 24 hrs by MTS assay Antiproliferative activity against p53-deficient human HCT116 cells after 24 hrs by MTS assay	[PMID: 24268795]
HCT-116	GI₅₀	55.7 μM Compound: Nutlin-3a	Antiproliferative activity against p53-deficient human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against p53-deficient human HCT116 cells after 48 hrs by MTT assay	[PMID: 24852275]
HCT-116	GI₅₀	8 μM Compound: Nutlin-3a	Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay	[PMID: 29089230]
HCT-116	GI₅₀	9 μM Compound: Nutlin-3a	Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis	[PMID: 29691156]
HCT-116	IC₅₀	9.07 μM Compound: 3	Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay	[PMID: 30045621]
HEK293	IC₅₀	> 50 μM Compound: Nutlin-3	Cytotoxicity against human HEK293 cells after 48 hrs by MTT assay Cytotoxicity against human HEK293 cells after 48 hrs by MTT assay	[PMID: 25618595]
HeLa	IC₅₀	27.5 μM Compound: Nutilin-3a; 9	Cytotoxicity against human HeLa cells harbouring unstable p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human HeLa cells harbouring unstable p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
HepG2	IC₅₀	10.2 μM Compound: Nutlin-3	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 23802716]
HepG2	IC₅₀	5.1 μM Compound: Nutlin-3a	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 25479770]
HepG2	GI₅₀	51.31 μM Compound: Nutlin-3	Antiproliferative activity against human HepG2 cells after 24 hrs by MTS assay Antiproliferative activity against human HepG2 cells after 24 hrs by MTS assay	[PMID: 24268795]
MCF7	IC₅₀	11.6 μM Compound: Nutlin-3	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 25618595]
MCF7	IC₅₀	2.9 μM Compound: Nutlin-3	Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 23802716]
MCF7	IC₅₀	3.74 μM Compound: Nutilin-3a; 9	Cytotoxicity against human MCF7 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human MCF7 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
MCF7	GI₅₀	48.74 μM Compound: Nutlin-3a	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 24852275]
MCF7	IC₅₀	5.01 μM Compound: Nutlin-3a	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 27101893]
MCF7	IC₅₀	8.5 μM Compound: 3	Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay	[PMID: 30045621]
MDA-MB-231	IC₅₀	23.5 μM Compound: Nutlin-3	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 25618595]
MDA-MB-435S	IC₅₀	29.6 μM Compound: Nutlin-3a	Antiproliferative activity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 27101893]
NCI-H1299	IC₅₀	10.4 μM Compound: Nutlin-3a	Antiproliferative activity against p53 -/- human NCI-H1299 cells incubated for 72 hrs by MTS assay Antiproliferative activity against p53 -/- human NCI-H1299 cells incubated for 72 hrs by MTS assay	[PMID: 30221935]
NCI-H1299	IC₅₀	14.7 μM Compound: Nutlin-3	Cytotoxicity against human H1299 cells after 72 hrs by CellTiterGlo luciferase-based assay Cytotoxicity against human H1299 cells after 72 hrs by CellTiterGlo luciferase-based assay	[PMID: 24139845]
NCI-H1299	IC₅₀	19.76 μM Compound: 3	Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay	[PMID: 30045621]
NCI-H1299	IC₅₀	20.4 μM Compound: Nutlin-3a	Antiproliferative activity against human p53-deficient NCI-H1299 cells after 72 hrs by MTT assay Antiproliferative activity against human p53-deficient NCI-H1299 cells after 72 hrs by MTT assay	[PMID: 22940704]
NCI-H1299	IC₅₀	20.48 μM Compound: Nutlin-3a	Antiproliferative activity against p53 deficient human NCI-H1299 cells after 72 hrs by MTT assay Antiproliferative activity against p53 deficient human NCI-H1299 cells after 72 hrs by MTT assay	[PMID: 23046248]
NCI-H460	IC₅₀	2.19 μM Compound: Nutilin-3a; 9	Cytotoxicity against human NCI-H460 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human NCI-H460 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
PC-3	IC₅₀	20.04 μM Compound: Nutlin-3	Cytotoxicity against human p53 deficient PC3 cells after 72 hrs by SRB assay Cytotoxicity against human p53 deficient PC3 cells after 72 hrs by SRB assay	[PMID: 23611770]
PC-3	IC₅₀	20.04 μM Compound: Nutlin-3	Cytotoxicity against human p53-null PC3 cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human p53-null PC3 cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 23601819]
PC-3	IC₅₀	30.3 μM Compound: Nutlin-3	Cytotoxicity against human PC3 cells after 24 hrs by MTT assay Cytotoxicity against human PC3 cells after 24 hrs by MTT assay	[PMID: 23802716]
RKO	IC₅₀	1.5 μM Compound: 1, Nutlin-3a	Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay	[PMID: 24900694]
RKO	IC₅₀	2.49 μM Compound: Nutilin-3a; 9	Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
SAOS-2	IC₅₀	12.1 μM Compound: Nutlin-3a	Antiproliferative activity against human p53-deficient Saos2 cells after 72 hrs by MTT assay Antiproliferative activity against human p53-deficient Saos2 cells after 72 hrs by MTT assay	[PMID: 22940704]
SAOS-2	GI₅₀	18 μM Compound: 1	Cytotoxicity against human Saos2 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human Saos2 cells after 72 hrs by sulforhodamine B assay	[PMID: 21314128]
SAOS-2	IC₅₀	31.62 μM Compound: Nutlin-3a	Antiproliferative activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay Antiproliferative activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay	[PMID: 23046248]
SAOS-2	IC₅₀	54.38 μM Compound: Nutlin-3a	Antitumor activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay Antitumor activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay	[PMID: 21996465]
SJSA-1	IC₅₀	0.7 μM Compound: Nutlin-3a	Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum	[PMID: 22524527]
SJSA-1	GI₅₀	1.3 μM Compound: 1	Growth inhibition of human SJSA1 cells expressing MDM2 by SRB assay Growth inhibition of human SJSA1 cells expressing MDM2 by SRB assay	[PMID: 21875801]
SJSA-1	IC₅₀	1.44 μM Compound: Nutlin-3a	Antiproliferative activity against human SJSA1 cells expressing wild type p53 incubated for 72 hrs by MTS assay Antiproliferative activity against human SJSA1 cells expressing wild type p53 incubated for 72 hrs by MTS assay	[PMID: 30221935]
SJSA-1	IC₅₀	1.5 μM Compound: 1, Nutlin-3a	Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay	[PMID: 24900694]
SJSA-1	IC₅₀	1.9 μM Compound: nutlin-3a	Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 72 hrs by CellTitre-Glo assay Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 72 hrs by CellTitre-Glo assay	[PMID: 26985323]
SJSA-1	GI₅₀	2.6 μM Compound: 1	Cytotoxicity against human SJSA1 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human SJSA1 cells after 72 hrs by sulforhodamine B assay	[PMID: 21314128]
SJSA-1	EC₅₀	22.8 μM Compound: Nutlin 3a	Cytotoxicity in human SJSA1 cells over expressing human DM2 after 24 hrs by CellTiter-Glo assay Cytotoxicity in human SJSA1 cells over expressing human DM2 after 24 hrs by CellTiter-Glo assay	[PMID: 29150077]
SJSA-1	EC₅₀	4.2 μM Compound: Nutlin-3a	Antiproliferative activity against human SJSA1 cells expressing wild-type p53 incubated for 72 hrs by MTT assay Antiproliferative activity against human SJSA1 cells expressing wild-type p53 incubated for 72 hrs by MTT assay	[PMID: 31657556]
SJSA-1	IC₅₀	7.1 μM Compound: Nutlin-3a	Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum	[PMID: 22524527]
SW480	IC₅₀	19.78 μM Compound: Nutilin-3a; 9	Cytotoxicity against human SW480 cells harbouring mutant p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human SW480 cells harbouring mutant p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
SW-620	GI₅₀	57.04 μM Compound: Nutlin-3	Antiproliferative activity against human SW620 cells expressing p53 mutant after 24 hrs by MTS assay Antiproliferative activity against human SW620 cells expressing p53 mutant after 24 hrs by MTS assay	[PMID: 24268795]
U2OS	IC₅₀	14.31 μM Compound: Nutlin-3a	Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay	[PMID: 23046248]
U2OS	IC₅₀	19.6 μM Compound: Nutlin-3a	Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay	[PMID: 22940704]
U2OS	IC₅₀	24.61 μM Compound: Nutlin-3a	Antitumor activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay Antitumor activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay	[PMID: 21996465]
U2OS	IC₅₀	3.35 μM Compound: Nutilin-3a; 9	Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
U-937	IC₅₀	15.6 μM Compound: Nutlin-3	Cytotoxicity against human U937 cells after 24 hrs by MTT assay Cytotoxicity against human U937 cells after 24 hrs by MTT assay	[PMID: 23802716]
Vero	IC₅₀	> 50 μM Compound: Nutlin-3	Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay	[PMID: 25618595]

体外研究
(In Vitro)

Nutlin-3a 可抑制 MDM2、激活野生型 p53 并诱导细胞凋亡，可作为 TP53 野生型卵巢癌的治疗化合物。三种具有野生型 TP53 的细胞系 (HOC-7、OVCA429 和 A2780) 对 Nutlin-3a 高度敏感 (IC₅₀=4 至 6 μM)。SKOV3 细胞对 Nutlin-3a 的 IC₅₀ 为 38 μM。其余两种卵巢透明细胞系（TOV21G 和 OVAS）均为 TP53 野生型，与 TP53 突变细胞系^[1]相比，它们对 Nutlin-3a 的生长抑制相对更敏感（IC₅₀ 分别为 14 和 25 μm）。Nutlin-3a 是 Nutlin-3 的活性对映体。Nutlin-3a 是一种高选择性 MDM2 拮抗剂和 p53 诱导剂。与 10 μM Nutlin-3a 孵育七天可抑制 NIH/3T3 细胞生长 90% 以上，但不影响 MEF 的增殖，因为药物的两个靶标均被消除。 Nutlin-3a 可有效抑制所有细胞系中的细胞周期进程，将 S 期区室消耗至 0.2-2%，并增加 G₁ 和 G₂/M 期区室，表明 G₁ 和 G₂ 停滞。添加 Nutlin-3a 3 小时后，p53 靶标 p21 和 MDM2 显著升高，并在 8 小时时达到最高水平。Nutlin-3a 在 40 小时后诱导约 60% 的 SJSA-1 和 MHM 细胞凋亡，60 小时后进一步增加（分别为 85% 和 65%）^[2]。

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

体内研究
(In Vivo)

Nutlin-3a 在所有模型中均有效，平均肿瘤生长抑制率≥98%。Nutlin-3a 以剂量依赖性方式抑制异种移植瘤生长，最高剂量（200 mg/kg）显示肿瘤明显缩小（8 次部分消退和 1 次完全消退）。使用 Nutlin-3a 建立的 SJSA-1 和 MHM 骨肉瘤异种移植瘤可导致大量肿瘤消退^[2]。

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

分子量

581.49

Formula

C₃₀H₃₀Cl₂N₄O₄

CAS 号

675576-98-4

性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (171.97 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7197 mL	8.5986 mL	17.1972 mL
5 mM	0.3439 mL	1.7197 mL	3.4394 mL
10 mM	0.1720 mL	0.8599 mL	1.7197 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制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

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.30 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.30 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.30 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制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

请依序添加每种溶剂： 50% PEG300 50% Saline
Solubility: 8 mg/mL (13.76 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.00%

选择批次：

Data Sheet (660 KB) SDS (392 KB)

COA (297 KB) HNMR (303 KB) LCMS (93 KB) 元素分析报告 (220 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Crane EK, et al. Nutlin-3a: A Potential Therapeutic Opportunity for TP53 Wild-Type Ovarian Carcinomas. PLoS One. 2015 Aug 6;10(8):e0135101. [Content Brief]

[2]. Tovar C, et al. Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy. Proc Natl Acad Sci U S A. 2006 Feb 7;103(6):1888-93. [Content Brief]

[3]. M Ulrich, et al. Murine tumor models for the in vivo evaluation of natural compounds and their derivatives as new cancer therapeutics. München. 2016.

Cell Assay ^[1]	All 15 cell lines are plated at a density of 1×10³ cells per well in 96-well plates. After 24h, media is exchanged and cells are treated with incremental concentrations of Nutlin 3a (1 μM, 5 μM, 10 μM, 25 μM, 50 μM, and 70 μM). After 72 h of incubation, WST-1 is added to each well, and a microplate reader is used at an absorbance of 450 nm to measure the number of remaining viable cells. Experiments are repeated with smaller titrations of Nutlin 3a as needed to determine the exact IC₅₀ of cell lines. The IC₅₀ is defined. Cell lines are again plated in a manner identical to above and treated with Nutlin 3a at their respective IC₅₀, and WST-1 is added with cell viability measurement at 24, 48, and 72h^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] Nude mice bearing s.c. tumor xenografts (10 mice per group in the SJSA-1, LnCaP, and 22Rv1 study and 15 mice per group in the MHM study) are dosed orally twice daily with Nutlin 3a (50-200 mg/kg) or vehicle (1% Klucel, 0.1% Tween 80) for 2 weeks (22Rv1 and LnCap) or 3 weeks (SJSA-1 and MHM). Tumor volume is measured with a caliper and calculated. For Western blot analysis, nude mice with established SJSA-1 tumors (200-400 mm³, three animals per group are treated with three doses of Nutlin 3a at 150 mg/kg (at 0, 8, and 24 h), and tumors are harvested 3 h after the last dose. Tumor samples are flash-frozen and processed^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Crane EK, et al. Nutlin-3a: A Potential Therapeutic Opportunity for TP53 Wild-Type Ovarian Carcinomas. PLoS One. 2015 Aug 6;10(8):e0135101. [Content Brief] [2]. Tovar C, et al. Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy. Proc Natl Acad Sci U S A. 2006 Feb 7;103(6):1888-93. [Content Brief] [3]. M Ulrich, et al. Murine tumor models for the in vivo evaluation of natural compounds and their derivatives as new cancer therapeutics. München. 2016.

Nutlin-3a 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7197 mL	8.5986 mL	17.1972 mL	42.9930 mL
	5 mM	0.3439 mL	1.7197 mL	3.4394 mL	8.5986 mL
	10 mM	0.1720 mL	0.8599 mL	1.7197 mL	4.2993 mL
	15 mM	0.1146 mL	0.5732 mL	1.1465 mL	2.8662 mL
	20 mM	0.0860 mL	0.4299 mL	0.8599 mL	2.1497 mL
	25 mM	0.0688 mL	0.3439 mL	0.6879 mL	1.7197 mL
	30 mM	0.0573 mL	0.2866 mL	0.5732 mL	1.4331 mL
	40 mM	0.0430 mL	0.2150 mL	0.4299 mL	1.0748 mL
	50 mM	0.0344 mL	0.1720 mL	0.3439 mL	0.8599 mL
	60 mM	0.0287 mL	0.1433 mL	0.2866 mL	0.7166 mL
	80 mM	0.0215 mL	0.1075 mL	0.2150 mL	0.5374 mL
	100 mM	0.0172 mL	0.0860 mL	0.1720 mL	0.4299 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:

Nutlin-3a675576-98-4RebemadlinMDM-2/p53E1/E2/E3 EnzymeAutophagyApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseovariancarcinomasp53Inhibitorinhibitorinhibit

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Nutlin-3a (Synonyms: Rebemadlin)

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MCE 顾客使用本产品发表的 47 篇科研文献

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Nutlin-3a (Synonyms: Rebemadlin)

Customer Review

Other Forms of Nutlin-3a:

Nutlin-3a 相关抗体

MCE 顾客使用本产品发表的 47 篇科研文献

Nutlin-3a 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

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参考文献

Nutlin-3a 相关抗体:

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