LB-100CAS# 1026680-07-8 |
- CUDC-101
Catalog No.:BCC2149
CAS No.:1012054-59-9
- Valproic acid sodium salt (Sodium valproate)
Catalog No.:BCC2156
CAS No.:1069-66-5
- M344
Catalog No.:BCC2162
CAS No.:251456-60-7
- Belinostat (PXD101)
Catalog No.:BCC2153
CAS No.:414864-00-9
- Trichostatin A (TSA)
Catalog No.:BCC3605
CAS No.:58880-19-6
- JNJ-26481585
Catalog No.:BCC2147
CAS No.:875320-29-9
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1026680-07-8 | SDF | Download SDF |
PubChem ID | 3578572 | Appearance | Powder |
Formula | C13H20N2O4 | M.Wt | 268.31 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble in DMSO | ||
Chemical Name | 2-(4-methylpiperazine-1-carbonyl)-7-oxabicyclo[2.2.1]heptane-3-carboxylic acid | ||
SMILES | CN1CCN(CC1)C(=O)C2C3CCC(C2C(=O)O)O3 | ||
Standard InChIKey | JUQMLSGOTNKJKI-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C13H20N2O4/c1-14-4-6-15(7-5-14)12(16)10-8-2-3-9(19-8)11(10)13(17)18/h8-11H,2-7H2,1H3,(H,17,18) | ||
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. |
LB-100 Dilution Calculator
LB-100 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 3.727 mL | 18.6352 mL | 37.2703 mL | 74.5406 mL | 93.1758 mL |
5 mM | 0.7454 mL | 3.727 mL | 7.4541 mL | 14.9081 mL | 18.6352 mL |
10 mM | 0.3727 mL | 1.8635 mL | 3.727 mL | 7.4541 mL | 9.3176 mL |
50 mM | 0.0745 mL | 0.3727 mL | 0.7454 mL | 1.4908 mL | 1.8635 mL |
100 mM | 0.0373 mL | 0.1864 mL | 0.3727 mL | 0.7454 mL | 0.9318 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. |
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
Auburn University
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
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
- RO-3
Catalog No.:BCC7548
CAS No.:1026582-88-6
- SC-10
Catalog No.:BCC6643
CAS No.:102649-79-6
- SC-9
Catalog No.:BCC6646
CAS No.:102649-78-5
- Pantoprazole
Catalog No.:BCC5432
CAS No.:102625-70-7
- Saprorthoquinone
Catalog No.:BCN3147
CAS No.:102607-41-0
- Ganoderic acid L
Catalog No.:BCN8204
CAS No.:102607-24-9
- Methyl lucidente G
Catalog No.:BCN8269
CAS No.:102607-20-5
- R788 disodium
Catalog No.:BCC3695
CAS No.:1025687-58-4
- 2,3,23-Trihydroxy-12-oleanen-28-oic acid
Catalog No.:BCN1638
CAS No.:102519-34-6
- (-)-Huperzine A
Catalog No.:BCN1057
CAS No.:102518-79-6
- SGI-1776 free base
Catalog No.:BCC2232
CAS No.:1025065-69-3
- Periglaucine B
Catalog No.:BCN7053
CAS No.:1025023-05-5
- Labd-13-ene-8,15-diol
Catalog No.:BCN5840
CAS No.:10267-31-9
- VX-222 (VCH-222, Lomibuvir)
Catalog No.:BCC2108
CAS No.:1026785-59-0
- H-Gln(Trt)-OH
Catalog No.:BCC2919
CAS No.:102747-84-2
- PSB 0788
Catalog No.:BCC7599
CAS No.:1027513-54-7
- Levetiracetam
Catalog No.:BCC1056
CAS No.:102767-28-2
- GYKI 52466 dihydrochloride
Catalog No.:BCC7072
CAS No.:102771-26-6
- [D-p-Cl-Phe6,Leu17]-VIP
Catalog No.:BCC5968
CAS No.:102805-45-8
- RuBi-GABA
Catalog No.:BCC6012
CAS No.:1028141-88-9
- Dihydrocinchonamine
Catalog No.:BCN5841
CAS No.:10283-68-8
- VUF 10460
Catalog No.:BCC6285
CAS No.:1028327-66-3
- BEZ235 Tosylate
Catalog No.:BCC1416
CAS No.:1028385-32-1
- D-Pinitol
Catalog No.:BCN5842
CAS No.:10284-63-6
LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation.[Pubmed:26666823]
Tumour Biol. 2016 Jun;37(6):7277-86.
Hepatocellular carcinoma (HCC) is a common cancer with poor prognosis. The multikinase inhibitor sorafenib is the only clinically proved systematic treatment for HCC. However, few patients respond to sorafenib. Hypoxic microenvironments contribute to sorafenib resistance. LB-100, a serine/threonine protein phosphatase 2A (PP2A) inhibitor was previously found to be a chemosensitizer in HCC. Here, we tested whether LB-100 could sensitize HCC to the effects of sorafenib. Intriguingly, LB-100 enhanced the effects of sorafenib in HCC cells only during hypoxic environments. LB-100 dramatically increased intracellular p-Smad3 level, which was responsible for the effect of LB-100 as a sensitizer. LB-100 downregulated Bcl-2 expression and enhanced sorafenib-induced apoptosis in HCC cells. We further proved that PP2A mediated LB-100-induced p-Smad3 overexpression. In addition, p38 mitogen-activated protein kinase pathway was activated in hypoxic conditions, and enhanced p-Smad3-dependent Bcl-2 inhibition and consequent apoptosis. In conclusion, LB-100 sensitized HCC cells to sorafenib in hypoxic environments. This effect was mediated by inactivation of PP2A, resulting in enhanced level of p-Smad3. Increased p-Smad3 downregulated Bcl-2, causing increased apoptosis of HCC cells.
Safety, Tolerability, and Preliminary Activity of LB-100, an Inhibitor of Protein Phosphatase 2A, in Patients with Relapsed Solid Tumors: An Open-Label, Dose Escalation, First-in-Human, Phase I Trial.[Pubmed:28039265]
Clin Cancer Res. 2017 Jul 1;23(13):3277-3284.
Purpose: To determine the MTD and to assess the safety, tolerability, and potential activity of LB-100, a first-in-class small-molecule inhibitor of protein phosphatase 2A (PP2A) in adult patients with progressive solid tumors.Experimental Design: LB-100 was administered intravenously daily for 3 days in 21-day cycles in a 3 + 3 dose escalation design.Results: There were 29 patient entries over 7 dose escalations. One patient stopped treatment after one dose because of an acute infection and was reenrolled after recovery; each course was analyzed as a separate patient entry. Two patients had dose-limiting toxicity (reversible increases in serum creatinine or calculated serum creatinine clearance) at the 3.1 mg/m(2) level. Probable or possible study drug-related grade 3 adverse events occurred in 6 (20.7%) patients [anemia (n = 2), decreased creatinine clearance, dyspnea, hyponatremia, and lymphopenia]. Ten (50%) of 20 response-evaluable patients had stable disease for four or more cycles. One patient with pancreatic adenocarcinoma had a partial response noted after 10 cycles, which was maintained for five additional cycles. The other patients achieving stable disease had one of the following: fibrosarcoma, chondrosarcoma, thymoma, atypical carcinoid of lung, or ovarian, testicular, breast (n = 2), and prostate cancer. The recommended phase II dose of LB-100 is 2.33 mg/m(2) daily for 3 days every 3 weeks.Conclusions: The safety, tolerability, preliminary evidence of antitumor activity, and novel mechanism of action of LB-100 support its continued development alone and in combination with other therapies. Clin Cancer Res; 23(13); 3277-84. (c)2016 AACR.