Nutlin-3a (Synonyms: Rebemadlin)

目錄號: HY-10029 純度: 99.00%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Nutlin-3a (Rebemadlin) 是 Nutlin-3 的活性對映體，是一種有效的 MDM2 抑制劑。Nutlin-3a 可抑制 MDM2-p53 相互作用，穩(wěn)定 p53 蛋白，從而誘導(dǎo)細胞自噬 (autophagy) 和凋亡 (apoptosis)。Nutlin-3a 有潛力用于 TP53 野生型卵巢癌的研究。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Nutlin-3a Chemical Structure

CAS No. : 675576-98-4

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規(guī)格	價格	是否有貨
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		詢價
500 mg		詢價

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Customer Review

Other Forms of Nutlin-3a:

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

MCE 顧客使用本產(chǎn)品發(fā)表的 47 篇科研文獻

•Cancer Cell. 2024 May 13;42(5):850-868.e9. [Abstract]
•Cell. 2024 Feb 1;187(3):712-732.e38. [Abstract]
•Cancer Cell. 2023 Oct 9;41(10):1731-1748.e8. [Abstract]
•Mol Cancer. 2024 Oct 30;23(1):242. [Abstract]
•Nat Immunol. 2023 May;24(5):780-791. [Abstract]
•Nat Commun. 2024 Oct 4;15(1):8624. [Abstract]

•J Adv Res. 2024 Jul 26:S2090-1232(24)00307-2. [Abstract]
•Adv Sci (Weinh). 2024 Jun 18:e2307751. [Abstract]
•Adv Sci (Weinh). 2024 Jun 10:e2401396. [Abstract]
•Cell Death Differ. 2022 Nov 12. [Abstract]
•Nat Commun. 2022 Aug 4;13(1):4534. [Abstract]
•Cell Death Differ. 2022 Apr 28. [Abstract]
•Dev Cell. 2022 Feb 23;S1534-5807(22)00079-X. [Abstract]
•EMBO J. 2022 Jan 5;e108946. [Abstract]
•EMBO J. 2020 Dec 22;e104844. [Abstract]
•Acta Pharmacol Sin. 2024 Oct 9. [Abstract]
•Proc Natl Acad Sci U S A. 2020 Jul 28;117(30):17808-17819. [Abstract]
•J Pharm Anal. 2024 Aug 22.
•Mol Oncol. 2022 Mar;16(5):1200-1217. [Abstract]
•Cell Rep. 2022 Aug 9;40(6):111177. [Abstract]
•Oncogenesis. 2022 Jul 2;11(1):37. [Abstract]
•Br J Pharmacol. 2021 Oct 2. [Abstract]
•Cell Rep. 2019 Apr 23;27(4):1176-1189.e5. [Abstract]
•J Mater Chem B. 2017, 5, 5816-5834.
•Cancer Sci. 2023 Sep 19. [Abstract]
•J Virol. 2023 May 23;e0037023. [Abstract]
•Lab Invest. 2023 Feb 7.
•Eur J Pharmacol. 2022 Jun 15;925:175002. [Abstract]
•Molecules. 2020 Mar 5;25(5):1162. [Abstract]
•J Cell Mol Med. 2020 Mar;24(6):3611-3624. [Abstract]
•Oral Oncol. 2019 Nov;98:53-61. [Abstract]
•Biochim Biophys Acta Mol Cell Res. 2019 Aug;1866(8):1272-1281. [Abstract]
•Eur J Med Chem. 2016 May 23;114:328-36. [Abstract]
•Adv Ther. 2024 Jul 18.
•Oncol Res. 2024 Mar 20;32(4):753-768. [Abstract]
•Med Oncol. 2022 Dec 16;40(1):49. [Abstract]
•R Soc Open Sci. 2018 Aug 29;5(8):172376. [Abstract]
•J Endocrinol. 2018 Apr;237(1):1-14. [Abstract]
•bioRxiv. 2024 Oct 9:2024.10.08.617155. [Abstract]
•biorxiv. 2024 Jun 13.
•Research Square Preprint. 2024 Mar 28.
•bioRxiv. 2023 Jul 27.
•Research Square Preprint. 2023 Jul 25.
•Research Square Preprint. 2023 May 25.
•bioRxiv. 2020 Jun.
•Biochim Biophys Acta. 2018 Apr 26;1865(8):1034-1045. [Abstract]
•University of Munich. 16. 2016 Jul.

: 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

Nutlin-3a 相關(guān)產(chǎn)品

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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

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]

細胞效力
(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]

體外研究
(In Vitro)

Nutlin-3a 可抑制 MDM2、激活野生型 p53 并誘導(dǎo)細胞凋亡，可作為 TP53 野生型卵巢癌的治療化合物。三種具有野生型 TP53 的細胞系 (HOC-7、OVCA429 和 A2780) 對 Nutlin-3a 高度敏感 (IC₅₀=4 至 6 μM)。SKOV3 細胞對 Nutlin-3a 的 IC₅₀ 為 38 μM。其余兩種卵巢透明細胞系（TOV21G 和 OVAS）均為 TP53 野生型，與 TP53 突變細胞系^[1]相比，它們對 Nutlin-3a 的生長抑制相對更敏感（IC₅₀ 分別為 14 和 25 μm）。Nutlin-3a 是 Nutlin-3 的活性對映體。Nutlin-3a 是一種高選擇性 MDM2 拮抗劑和 p53 誘導(dǎo)劑。與 10 μM Nutlin-3a 孵育七天可抑制 NIH/3T3 細胞生長 90% 以上，但不影響 MEF 的增殖，因為藥物的兩個靶標(biāo)均被消除。 Nutlin-3a 可有效抑制所有細胞系中的細胞周期進程，將 S 期區(qū)室消耗至 0.2-2%，并增加 G₁ 和 G₂/M 期區(qū)室，表明 G₁ 和 G₂ 停滯。添加 Nutlin-3a 3 小時后，p53 靶標(biāo) p21 和 MDM2 顯著升高，并在 8 小時時達到最高水平。Nutlin-3a 在 40 小時后誘導(dǎo)約 60% 的 SJSA-1 和 MHM 細胞凋亡，60 小時后進一步增加（分別為 85% 和 65%）^[2]。

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

體內(nèi)研究
(In Vivo)

Nutlin-3a 在所有模型中均有效，平均腫瘤生長抑制率≥98%。Nutlin-3a 以劑量依賴性方式抑制異種移植瘤生長，最高劑量（200 mg/kg）顯示腫瘤明顯縮小（8 次部分消退和 1 次完全消退）。使用 Nutlin-3a 建立的 SJSA-1 和 MHM 骨肉瘤異種移植瘤可導(dǎo)致大量腫瘤消退^[2]。

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

分子量

581.49

Formula

C₃₀H₃₀Cl₂N₄O₄

CAS 號

675576-98-4

性狀

固體

顏色

White to light yellow

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : ≥ 100 mg/mL (171.97 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)

* "≥" 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	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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(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(dāng)?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(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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: ≥ 2.5 mg/mL (4.30 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 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: 2.5 mg/mL (4.30 mM); 懸濁液; 超聲助溶

此方案可獲得 2.5 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 25.0 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。
方案三

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.30 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

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： 50% PEG300 50% Saline
Solubility: 8 mg/mL (13.76 mM); 澄清溶液; 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(jié)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(shù)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(jǐn)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: 99.00%

選擇批次：

Data Sheet (660 KB) SDS (392 KB)

COA (297 KB) HNMR (303 KB) LCMS (93 KB) 元素分析報告 (220 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻

[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.
參考文獻	[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 相關(guān)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

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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