PM00104

CAS# 308359-57-1

PM00104

Catalog No. BCC4237----Order now to get a substantial discount!

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Quality Control of PM00104

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Chemical structure

PM00104

3D structure

Chemical Properties of PM00104

Cas No. 308359-57-1 SDF Download SDF
PubChem ID 16061448 Appearance Powder
Formula C37H38F3N3O8 M.Wt 709.71
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
SMILES CC1=C(C(=C2C3C4CC5=C(C(N4C(C(N3C)CC2=C1)O)CNC(=O)C=CC6=CC(=CC=C6)C(F)(F)F)C7=C(C(=C5OC(=O)C)C)OCO7)O)OC
Standard InChIKey VPAHZSUNBOYNQY-DLVGLDQCSA-N
Standard InChI InChI=1S/C37H38F3N3O8/c1-17-11-21-13-25-36(47)43-24(30(42(25)4)28(21)31(46)32(17)48-5)14-23-29(35-34(49-16-50-35)18(2)33(23)51-19(3)44)26(43)15-41-27(45)10-9-20-7-6-8-22(12-20)37(38,39)40/h6-12,24-26,30,36,46-47H,13-16H2,1-5H3,(H,41,45)/b10-9+/t24-,25-,26-,30-,36-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

PM00104 Dilution Calculator

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PM00104 Molarity Calculator

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Preparing Stock Solutions of PM00104

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.409 mL 7.0451 mL 14.0903 mL 28.1805 mL 35.2257 mL
5 mM 0.2818 mL 1.409 mL 2.8181 mL 5.6361 mL 7.0451 mL
10 mM 0.1409 mL 0.7045 mL 1.409 mL 2.8181 mL 3.5226 mL
50 mM 0.0282 mL 0.1409 mL 0.2818 mL 0.5636 mL 0.7045 mL
100 mM 0.0141 mL 0.0705 mL 0.1409 mL 0.2818 mL 0.3523 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

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Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
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Universite de Paris
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Auckland University
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The University of Tokyo
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Korea University
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Background on PM00104

Zalypsis(PM00104) is an alkaloid analog to certain natural marine compound. Zalyps is a potent antimyeloma agent with IC50 values from picomolar to low nanomolar ranges.

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References on PM00104

PM00104 (Zalypsis(R)): a marine derived alkylating agent.[Pubmed:25153860]

Molecules. 2014 Aug 15;19(8):12328-35.

PM00104 (Zalypsis(R)) is a synthethic tetrahydroisoquinolone alkaloid, which is structurally similar to many marine organisms. The compound has been proposed as a potential chemotherapeutic agent in the treatment of solid human tumors and hematological malignancies. PM00104 is a DNA binding agent, causing inhibition of the cell cycle and transcription, which can lead to double stranded DNA breaks. After rigorous pre-clinical testing, the drug has been evaluated in a number of phase II clinical trials. This manuscript provides a review of current trials and appraises the efficacy of PM00104 as a future cancer treatment.

Phase II clinical trial of PM00104 (Zalypsis((R))) in urothelial carcinoma patients progressing after first-line platinum-based regimen.[Pubmed:24570330]

Cancer Chemother Pharmacol. 2014 Apr;73(4):857-67.

PURPOSE: This exploratory phase II clinical trial evaluated the antitumor activity, safety profile and pharmacokinetics of PM00104 (Zalypsis((R))) 3 mg/m(2) 1 h every 3-week intravenous infusion in patients with advanced and/or metastatic urothelial carcinoma progressing after first-line platinum-based chemotherapy. METHODS: The primary efficacy end point was the disease control rate (DCR), defined as the percentage of patients with confirmed objective response or progression-free at 3 months, according to the response evaluation criteria in solid tumors. RESULTS: In a first stage (n = 19 patients evaluable for efficacy), only one patient achieved DCR (stable disease as best response and progression-free survival of 3.1 months). According to the 2-stage design used, the primary efficacy objective was unmet, and therefore, the trial was finalized without opening the second stage. The most common adverse events related to PM00104 were fatigue, anorexia, nausea, troponin I increase and neutropenia, which were transient and manageable with dose modifications or administration delays. Mean PK results (Cmax = 48.57 mug/l and area under the curve (AUC) = 154.97 h mug/l) were similar to those observed in a previous phase I trial evaluating the same dose and schedule. Few troponin I concentrations were higher than 0.10 ng/ml, and none of them were related to parameters of PM00104 exposure such as AUC or Cmax. CONCLUSIONS: No recommendation is given for further evaluation of PM00104 as single-agent treatment of patients with pretreated advanced and/or metastatic urothelial carcinoma. No new safety signals were observed.

Phase I study of carboplatin in combination with PM00104 (Zalypsis(R)) in patients with advanced solid tumors.[Pubmed:24535315]

Invest New Drugs. 2014 Aug;32(4):644-52.

This phase I trial determined the recommended dose for phase II trials (RD) of carboplatin 1-h intravenous (i.v.) infusion followed by PM00104 1-h i.v. infusion on Day 1 every 3 weeks (q3wk) in adult patients with advanced solid tumors. A toxicity-guided, dose-escalation design was used. Patients were stratified and divided into heavily (n = 6) or mildly pretreated (n = 14) groups. Transient grade 4 thrombocytopenia (in one heavily and three mildly pretreated patients) was the only dose-limiting toxicity (DLT) observed. Carboplatin AUC3-PM00104 2.0 mg/m(2) was the RD in both groups. At this RD, the carboplatin AUC was equal to ~60 % the target AUC used in other combinations, and the PM00104 dose intensity was 56-67 % of the value achieved at the RD for single-agent PM00104 given as 1-h infusion q3wk. Most treatment-related adverse events were grade 1/2. They mainly consisted of gastrointestinal and general symptoms, such as fatigue, anorexia, mucosal inflammation or nausea. Transient neutropenia (50 % of patients) and thrombocytopenia (33-38 %) were the most common severe hematological abnormalities; their incidence was higher than with single-agent PM00104. No pharmacokinetic drug-drug alterations occurred. Partial response was found in one patient with triple negative breast cancer pretreated with paclitaxel/bevacizumab. Three patients with colorectal cancer, head and neck cancer, and tumor of unknown origin had disease stabilization for >/=3 months. In conclusion, no optimal dose was reached due to overlapping myelosuppression despite stratification according to prior treatment. Therefore, this carboplatin plus PM00104 combination was not selected for further clinical research.

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