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Plitidepsin

Product Name
Plitidepsin
CAS No.
137219-37-5
Chemical Name
Plitidepsin
Synonyms
Aplidin;Plitidepsin;Plitidepsin top3;cyclic peptide deriv.;Plitidepsin (Aplidine);Didemnin A, N-(1-(1,2-dioxopropyl)-L-prolyl)-;2-9-Didemnin B, 2-(1-(1,2-dioxopropyl)-L-proline)-;Inhibitor,DNA/RNA Synthesis,MOLT-4,SARS coronavirus,infection,SARS-CoV,Plitidepsin,Leukemia,VEGF,COVID-19,Antiviral,inhibit,Aplidine,advanced cancer,anticancer,Advanced Malignancies;3,6-Anhydro-(N-{(2S,4S)-4-[(3S,4R,5S)-3-hydroxy-4-{[N-(2-oxo-propanoyl)-L-prolyl-N-Methyl-D-leucyl-L-threonyl]aMino}-5-Methyl-heptanoyloxy]-2,5-diMethyl-3-oxohexanoyl}-L-leucyl-L-prolyl-N;L-Tyrosine, 1-(1,2-dioxopropyl)-L-prolyl-N-methyl-D-leucyl-L-threonyl-(3S,4R,5S)-4-amino-3-hydroxy-5-methylheptanoyl-(2S,4S)-4-hydroxy-2,5-dimethyl-3-oxohexanoyl-L-leucyl-L-prolyl-N,o-dimethyl-, (8-3)-lactone
CBNumber
CB11508609
Molecular Formula
C57H87N7O15
Formula Weight
1110.34
MOL File
137219-37-5.mol
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Plitidepsin Property

Melting point:
152-160°
alpha 
D -95.9° (c = 1.8 in CHCl3)
Density 
1.24±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
DMSO: soluble
pka
11.28±0.70(Predicted)
InChIKey
UUSZLLQJYRSZIS-NIORUGPLNA-N
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H225Highly Flammable liquid and vapour

H319Causes serious eye irritation

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P233Keep container tightly closed.

P240Ground/bond container and receiving equipment.

P241Use explosion-proof electrical/ventilating/lighting/…/equipment.

P242Use only non-sparking tools.

P243Take precautionary measures against static discharge.

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P337+P313IF eye irritation persists: Get medical advice/attention.

P370+P378In case of fire: Use … for extinction.

P403+P235Store in a well-ventilated place. Keep cool.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

American Custom Chemicals Corporation
Product number
API0005125
Product name
APLIDINE
Purity
95.00%
Packaging
5MG
Price
$499.63
Updated
2021/12/16
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Plitidepsin Chemical Properties,Usage,Production

Description

Plitidepsin is a cyclic depsipeptide that was first isolated from a Mediterranean marine tunicate (Aplidium albicans) and, at present, is manufactured by total synthesis and commercialized as Aplidin?. Its antitumor activity, observed in preclinical in vitro and in vivo studies has prompted numerous clinical trials to be conducted over the last 17 years, alone or in combination with other anticancer agents.

Definition

ChEBI: Plitidepsin is a didemnin that is didemin B in which the hydroxy group of the 1-(2-hydroxypropanoyl)-L-prolinamide moiety has been oxidised to the corresponding ketone. It was originally isolated from the Mediterranean tunicate Aplidium albicans. It has a role as a marine metabolite, an antineoplastic agent and an anticoronaviral agent.

Biological Activity

Plitidepsin is a cytotoxic peptide originally found in the sea squirt Aplidium albicans. It interacts with a protein (eEF1A2) which is overexpressed in some cancers. This interaction leads to apoptosis. Synthetically produced plitidepsin has been found to have antiproliferative effects on cancer cells. Phase II trials have investigated its activity in tumours such as lung cancer, melanoma and multiple myeloma.

Mechanism of action

Plitidepsin induces apoptosis in multiple myeloma cells, which involves activation of p38 and c-jun NH(2)-terminal kinase signaling, Fas/CD95 translocation to lipid rafts, and ultimately caspase activation. The investigational agent also decreases the proliferation of multiple myeloma cells, an effect mediated by the suppression of several proliferative genes.In a pivotal phase III trial of patients with relapsed or refractory multiple myeloma, plitidepsin in combination with dexamethasone (Dex) significantly reduced the risk of progression or death compared to Dex alone.Plitidepsin has been approved by TGA in Australia for the treatment of multiple myeloma in combination with dexamethasone for patients that relapse after three lines of treatment, including proteasome inhibitors or immunomodulators.

Clinical Use

Plitidepsin is a cyclic depsipeptide isolated from the marine tunicate Aplidium albicans. Plitidepsin displays a broad spectrum of antitumor activities, inducing apoptosis by triggering mitochondrial cytochrome c release, initiating the Fas/ DC95, JNK pathway and activating caspase 3 activation. This agent also inhibits elongation factor 1-a, thereby interfering with protein synthesis, and induces G1 arrest and G2 blockade, thereby inhibiting tumor cell growth.A phase II prospective open-label study (Ferme et al. 2008 ) to evaluate its activity in patients with relapsed/ refractory non-cutaneous PTCL was conducted in 14 patients. They were treated with plitidepsin 3.2 mg/m 2 IV infusion over 1-h on days 1, 8 and 15 every 4 weeks. Eleven patients were evaluable when preliminary results were reported, one was too early and two were non-evaluable. One con fi rmed CR and 3 PR’s were observed with a 36% objective response rate. Median overall survival was 11 months.
Plitidepsin was tolerable in this heavily pretreated population with low hematological toxicity. Transient but reversible ALT elevation was noticed in 7 patients.
Future trials will establish its role in T-cell lymphoma.

in vitro

In vitro studies have demonstrated that plitidepsin has anti-myeloma activity against 19 multiple myeloma cell lines including cells resistant to anti-myeloma agents frequently used in the clinic (i.e. melphalan, doxorubicin, thalidomide derivatives, and dexamethasone) and primary multiple myeloma cells isolated from patients (13 out 16 showed a response to plitidepsin).

Plitidepsin Preparation Products And Raw materials

Raw materials

Preparation Products

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Plitidepsin Suppliers

Fuxin Pharmaceutical
Tel
021-50872116 13611907556
Fax
021-31300828
Email
contact@fuxinpharm.com
Country
China
ProdList
1575
Advantage
58
Alabiochem Tech.Co., Ltd.
Tel
0512-58900862 400-0707518
Fax
0086-512-56765862
Email
sales@alabiochem.com
Country
China
ProdList
995
Advantage
59
T&W GROUP
Tel
021-61551611 13296011611
Fax
+86 21-50676805
Email
contact@trustwe.com
Country
China
ProdList
9900
Advantage
58
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1494
Advantage
55
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3404
Advantage
58
Sichuan Wei Keqi Biological Technology Co., Ltd.
Tel
028-81700200 18116577057
Fax
028-81705658
Email
3003855609@qq.com
Country
China
ProdList
7893
Advantage
56
Taizhou KEDE Chemical Co., Ltd
Tel
0576-84613060 13093829633
Fax
0576-84613060
Email
sales@kedechemical.com
Country
China
ProdList
298
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Alfa Chemistry
Tel
1-516-6625404
Fax
1-516-927-0118
Email
support@alfa-chemistry.com
Country
United States
ProdList
9171
Advantage
60
Shanghai Synchem Pharma Co., ltd
Tel
021-61984905-1 18016477331
Email
synchempharma@aliyun.com
Country
China
ProdList
6451
Advantage
55
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View Lastest Price from Plitidepsin manufacturers

BOC Sciences
Product
Plitidepsin 137219-37-5
Price
US $998.00/mg
Min. Order
1mg
Purity
97%
Supply Ability
10mg
Release date
2021-05-07

137219-37-5, PlitidepsinRelated Search:


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  • Plitidepsin
  • 2-9-Didemnin B, 2-(1-(1,2-dioxopropyl)-L-proline)-
  • Aplidin
  • Didemnin A, N-(1-(1,2-dioxopropyl)-L-prolyl)-
  • L-Tyrosine, 1-(1,2-dioxopropyl)-L-prolyl-N-methyl-D-leucyl-L-threonyl-(3S,4R,5S)-4-amino-3-hydroxy-5-methylheptanoyl-(2S,4S)-4-hydroxy-2,5-dimethyl-3-oxohexanoyl-L-leucyl-L-prolyl-N,o-dimethyl-, (8-3)-lactone
  • 3,6-Anhydro-(N-{(2S,4S)-4-[(3S,4R,5S)-3-hydroxy-4-{[N-(2-oxo-propanoyl)-L-prolyl-N-Methyl-D-leucyl-L-threonyl]aMino}-5-Methyl-heptanoyloxy]-2,5-diMethyl-3-oxohexanoyl}-L-leucyl-L-prolyl-N
  • cyclic peptide deriv.
  • Plitidepsin (Aplidine)
  • Plitidepsin top3
  • Inhibitor,DNA/RNA Synthesis,MOLT-4,SARS coronavirus,infection,SARS-CoV,Plitidepsin,Leukemia,VEGF,COVID-19,Antiviral,inhibit,Aplidine,advanced cancer,anticancer,Advanced Malignancies
  • 137219-37-5
  • C57H87N7O15