Rocaglamide (Rocaglamide A) (Synonyms: Rocaglamide A; Roc-A)

Name: Rocaglamide (Rocaglamide A)
Brand: GlpBio
SKU: GC33426
Availability: InStock
Rating: 5 (39 reviews)

Katalog-Nr.GC33426

Rocaglamid (Rocaglamid A) (Roc-A) wird aus der Gattung Aglaia isoliert und kann bei Husten, Verletzungen, Asthma und entzÜndlichen Hauterkrankungen eingesetzt werden. Rocaglamid (Rocaglamid A) ist ein starker Inhibitor der NF-&7#954;B-Aktivierung in T-Zellen. Rocaglamid (Rocaglamid A) ist ein wirksamer und selektiver Hemmer der Aktivierung des Hitzeschockfaktors 1 (HSF1) mit einem IC50 von ~50 nM. Rocaglamid (Rocaglamid A) hemmt die Funktion des Translationsinitiationsfaktors eIF4A. Rocaglamid (Rocaglamid A) hat auch krebshemmende Eigenschaften bei LeukÄmie.

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Rocaglamide (Rocaglamide A) Chemische Struktur

Cas No.: 84573-16-0

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10mM (in 1mL DMSO)	511,00 $	Auf Lager
500μg	115,00 $	Auf Lager
1mg	185,00 $	Auf Lager
5mg	459,00 $	Auf Lager
10mg	783,00 $	Auf Lager

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Sample solution is provided at 25 µL, 10mM.

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Description Protocol Chemical Properties Product Documents

Product Documents

Quality Control & SDS

View current batch:

Purity: >98.50%

Protocol

Cell experiment [1]:
Cell lines	HepG2 and Huh-7 cells
Preparation Method	HepG2 and Huh-7 cells were seeded in 96-well plates in complete culture medium and incubated for 24 h. The cells were then exposed to 100 nM Rocaglamide (Rocaglamide A) and TRAIL for 24 h.
Reaction Conditions	100 nM;24h
Applications	Rocaglamide (Rocaglamide A) significantly enhanced TRAIL induced apoptosis.
Animal experiment [2]:
Animal models	Female SCID mice (6-week-old)
Preparation Method	The Huh-7 cells, suspended in 100 µl mix, were implanted subcutaneously into the right flank of 10 female SCID mice (6-week-old) and then randomly divided into two equal groups, one of which received an intraperitoneal injection of Rocaglamide (Rocaglamide A) (2.5 mg/kg in 80 µl olive oil; n=5) and the other, used as a vehicle contro. These treatments were performed once daily for 32 days and the tumor volumes and body weights of the animals were measured twice a week.
Dosage form	2.5 mg/kg; i.p.; 32 days
Applications	Rocaglamide (Rocaglamide A) induced tumor cell apoptosis in a SCID mouse model (Huah-7 cells) without causing weight loss in mice, and no significant signs of toxicity were observed during treatment, suggesting that Rocaglamide is generally well tolerated in vivo.
References: [1]. Luan Z, He Y, et,al. Rocaglamide overcomes tumor necrosis factor-related apoptosis-inducing ligand resistance in hepatocellular carcinoma cells by attenuating the inhibition of caspase-8 through cellular FLICE-like-inhibitory protein downregulation. Mol Med Rep. 2015 Jan;11(1):203-11. doi: 10.3892/mmr.2014.2718. Epub 2014 Oct 21. PMID: 25333816; PMCID: PMC4237083.

Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia (family Meliaceae). Rocaglamide (Rocaglamide A)(IC50 of 50 nM) inhibits the function of the translation initiation factor eIF4A, a DEAD box RNA helicase ^[1，2].

Rocaglamide (Rocaglamide A) (100 nM;24h) significantly enhanced TRAIL induced apoptosis^[4]. Rocaglamide (Rocaglamide A) (20- 100 nM;48h)can induce 10-30% apoptosis of L1236 and KM-H2 cells ^[3]. Rocaglamide (Rocaglamide A) are able to suppress the PMA-induced expression of NF-kappaB target genes and sensitize leukemic T cells to apoptosis induced by TNFalpha, cisplatin, and gamma-irradiation ^[5]. Rocaglamide (Rocaglamide A)( 30/50 nM;21d) prevented TNF-α mediated inhibition of osteoblast differentiation, and promoted osteoblast differentiation directly, in both C2C12 and primary mesenchymal stromal cells ^[6].

Rocaglamide (Rocaglamide A)( 2.5 mg/kg; i.p.; 32 days) induced tumor cell apoptosis in a SCID mouse model (Huah-7 cells) without causing weight loss in mice, and no significant signs of toxicity were observed during treatment, suggesting that Rocaglamide is generally well tolerated in vivo^[4]. Rocaglamide (Rocaglamide A)( 0.5 mg/kg; i.p.; five times per week for two weeks) overcomes CPT resistance in U266 in vitro and significant increases in anti-tumor efficacies of CPT in mice xenografted with U266^[7].

References:
[1]. Santagata S, Mendillo ML, et,al. Tight coordination of protein translation and HSF1 activation supports the anabolic malignant state. Science. 2013 Jul 19;341(6143):1238303. doi: 10.1126/science.1238303. PMID: 23869022; PMCID: PMC3959726.
[2]. Kim S, Salim AA, Swanson SM and Kinghorn AD: Potential of cyclopenta[b]benzofurans from Aglaia species in cancer chemotherapy. Anticancer Agents Med Chem. 6:319-345. 2006.
[3]. Giaisi M, KÖhler R, et,al. Rocaglamide and a XIAP inhibitor cooperatively sensitize TRAIL-mediated apoptosis in Hodgkin's lymphomas. Int J Cancer. 2012 Aug 15;131(4):1003-8. doi: 10.1002/ijc.26458. Epub 2011 Nov 8. PMID: 21952919.
[4]. Luan Z, He Y, et,al. Rocaglamide overcomes tumor necrosis factor-related apoptosis-inducing ligand resistance in hepatocellular carcinoma cells by attenuating the inhibition of caspase-8 through cellular FLICE-like-inhibitory protein downregulation. Mol Med Rep. 2015 Jan;11(1):203-11. doi: 10.3892/mmr.2014.2718. Epub 2014 Oct 21. PMID: 25333816; PMCID: PMC4237083.
[5]. Baumann B, Bohnenstengel F, et,al. Rocaglamide derivatives are potent inhibitors of NF-kappa B activation in T-cells. J Biol Chem. 2002 Nov 22;277(47):44791-800. doi: 10.1074/jbc.M208003200. Epub 2002 Sep 16. PMID: 12237314.
[6]. Li A, Yang L, et,al. Rocaglamide-A Potentiates Osteoblast Differentiation by Inhibiting NF-κB Signaling. Mol Cells. 2015 Nov;38(11):941-9. doi: 10.14348/molcells.2015.2353. Epub 2015 Nov 6. PMID: 26549505; PMCID: PMC4673408.
[7]. Wu Y, Giaisi M, et,al. Rocaglamide breaks TRAIL-resistance in human multiple myeloma and acute T-cell leukemia in vivo in a mouse xenogtraft model. Cancer Lett. 2017 Mar 28;389:70-77. doi: 10.1016/j.canlet.2016.12.010. Epub 2016 Dec 18. PMID: 27998762.

Cas No.	84573-16-0	SDF
Überlieferungen	Rocaglamide A; Roc-A
Canonical SMILES	O1C2=CC(OC)=CC(OC)=C2[C@]2(O)[C@H](O)[C@H](C(N(C)C)=O)[C@@H](C3=CC=CC=C3)[C@]12C1=CC=C(OC)C=C1 \|&1:11,13,15,21,28,r\|
Formula	C₂₉H₃₁NO₇	M.Wt	505.56
Löslichkeit	150 mg/mL in DMSO	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	1.978 mL	9.89 mL	19.78 mL
	5 mM	0.3956 mL	1.978 mL	3.956 mL
	10 mM	0.1978 mL	0.989 mL	1.978 mL

Molaritätsrechner
Verdünnung-Rechner

Berechnen

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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Rocaglamide (Rocaglamide A) (Synonyms: Rocaglamide A; Roc-A)

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GlpBio Citations

Bioactive Compounds Premium Provider

GlpBio Produkte in seriösen Veröffentlichungen zitiert

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

Molaritätsrechner

Verdünnung-Rechner

In vivo Formulation Calculator (Clear solution)

Bewertungen

Rocaglamide (Rocaglamide A) (Synonyms: Rocaglamide A; Roc-A)

Kundenbewertungen

GlpBio Citations

Bioactive Compounds Premium Provider

GlpBio Produkte in seriösen Veröffentlichungen zitiert

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

Molaritätsrechner

Verdünnung-Rechner

In vivo Formulation Calculator (Clear solution)

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