LB-100
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MedKoo CAT#: 206834

CAS#: 1632032-53-1

Description: LB-100 is a protein phosphatase 2A(PP2A)inhibitor. LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation. 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.


Price and Availability

Size
Price

10mg
USD 150
500mg
USD 1950
Size
Price

50mg
USD 450
1g
USD 2950
Size
Price

100mg
USD 750
5g
USD 6950

LB-100, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206834
Name: LB-100
CAS#: 1632032-53-1
Chemical Formula: C13H20N2O4
Exact Mass: 268.1423
Molecular Weight: 268.313
Elemental Analysis: C, 58.19; H, 7.51; N, 10.44; O, 23.85


Related CAS #: 1632032-53-1   1026680-07-8 (deleted)    

Synonym: LB-100; LB 100; LB100.

IUPAC/Chemical Name: 3-[(4-Methylpiperazin-1-yl)carbonyl]-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid

InChi Key: JUQMLSGOTNKJKI-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(C1C(O2)CCC2C1C(N3CCN(C)CC3)=O)O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Fu QH, Zhang Q, Zhang JY, Sun X, Lou Y, Li GG, Chen ZL, Bai XL, Liang TB. LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation. Tumour Biol. 2016 Jun;37(6):7277-86. doi: 10.1007/s13277-015-4560-2. Epub 2015 Dec 14. PubMed PMID: 26666823.

2: Chung V, Mansfield AS, Braiteh F, Richards D, Durivage H, Ungerleider RS, Johnson F, Kovach JS. 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. Clin Cancer Res. 2016 Dec 30. doi: 10.1158/1078-0432.CCR-16-2299. [Epub ahead of print] PubMed PMID: 28039265.

3: Bai XL, Zhang Q, Ye LY, Hu QD, Fu QH, Zhi X, Su W, Su RG, Ma T, Chen W, Xie SZ, Chen CL, Liang TB. Inhibition of protein phosphatase 2A enhances cytotoxicity and accessibility of chemotherapeutic drugs to hepatocellular carcinomas. Mol Cancer Ther. 2014 Aug;13(8):2062-72. doi: 10.1158/1535-7163.MCT-13-0800. Epub 2014 May 27. PubMed PMID: 24867249.

4: Bai X, Zhi X, Zhang Q, Liang F, Chen W, Liang C, Hu Q, Sun X, Zhuang Z, Liang T. Inhibition of protein phosphatase 2A sensitizes pancreatic cancer to chemotherapy by increasing drug perfusion via HIF-1α-VEGF mediated angiogenesis. Cancer Lett. 2014 Dec 28;355(2):281-7. doi: 10.1016/j.canlet.2014.09.048. Epub 2014 Oct 7. PubMed PMID: 25304380.

5: Nyholm D, Lewander T, Gomes-Trolin C, Bäckström T, Panagiotidis G, Ehrnebo M, Nyström C, Aquilonius SM. Pharmacokinetics of levodopa/carbidopa microtablets versus levodopa/benserazide and levodopa/carbidopa in healthy volunteers. Clin Neuropharmacol. 2012 May-Jun;35(3):111-7. doi: 10.1097/WNF.0b013e31825645d1. PubMed PMID: 22549097.

6: Lecca S, Pelosi A, Tchenio A, Moutkine I, Lujan R, Hervé D, Mameli M. Rescue of GABAB and GIRK function in the lateral habenula by protein phosphatase 2A inhibition ameliorates depression-like phenotypes in mice. Nat Med. 2016 Mar;22(3):254-61. doi: 10.1038/nm.4037. Epub 2016 Jan 25. PubMed PMID: 26808347.

7: Zhang C, Hong CS, Hu X, Yang C, Wang H, Zhu D, Moon S, Dmitriev P, Lu J, Chiang J, Zhuang Z, Zhou Y. Inhibition of protein phosphatase 2A with the small molecule LB100 overcomes cell cycle arrest in osteosarcoma after cisplatin treatment. Cell Cycle. 2015;14(13):2100-8. doi: 10.1080/15384101.2015.1041693. Epub 2015 May 5. PubMed PMID: 25942376; PubMed Central PMCID: PMC4612123.

8: Gordon IK, Lu J, Graves CA, Huntoon K, Frerich JM, Hanson RH, Wang X, Hong CS, Ho W, Feldman MJ, Ikejiri B, Bisht K, Chen XS, Tandle A, Yang C, Arscott WT, Ye D, Heiss JD, Lonser RR, Camphausen K, Zhuang Z. Protein Phosphatase 2A Inhibition with LB100 Enhances Radiation-Induced Mitotic Catastrophe and Tumor Growth Delay in Glioblastoma. Mol Cancer Ther. 2015 Jul;14(7):1540-7. doi: 10.1158/1535-7163.MCT-14-0614. Epub 2015 May 4. PubMed PMID: 25939762; PubMed Central PMCID: PMC4497833.

9: Hong CS, Ho W, Zhang C, Yang C, Elder JB, Zhuang Z. LB100, a small molecule inhibitor of PP2A with potent chemo- and radio-sensitizing potential. Cancer Biol Ther. 2015;16(6):821-33. doi: 10.1080/15384047.2015.1040961. Epub 2015 Apr 21. Review. PubMed PMID: 25897893; PubMed Central PMCID: PMC4623051.

10: Chang KE, Wei BR, Madigan JP, Hall MD, Simpson RM, Zhuang Z, Gottesman MM. The protein phosphatase 2A inhibitor LB100 sensitizes ovarian carcinoma cells to cisplatin-mediated cytotoxicity. Mol Cancer Ther. 2015 Jan;14(1):90-100. doi: 10.1158/1535-7163.MCT-14-0496. Epub 2014 Nov 5. PubMed PMID: 25376608; PubMed Central PMCID: PMC4557740.

11: Lembo M, Cannatà V, Militello A, Ritrovato M, Zaffina S, Derrico P, Borra M. [Artificial lighting and blue light in the operating room: what risks for the surgeon?]. Med Lav. 2015 Sep 9;106(5):342-50. Italian. PubMed PMID: 26384260.

12: Vaillant A, Dentan G, Laurent Y, Aurélie G, Beer JC, Germin F, Boch É, Casillas JM, Brunel P, Touzery C, Cottin Y, Zeller M, Morel G; pour le réseau de prise en charge et de prévention des infarctus du myocarde de Côte-d’Or (RPC-PIM).. The Log book for the secondary prevention of coronary artery disease: A pilot study. Presse Med. 2015 Sep;44(9):e301-9. doi: 10.1016/j.lpm.2014.11.020. Epub 2015 Jul 2. PubMed PMID: 26144276.

13: Broadhurst T, Huang X, Frye B, Ellis R. A Spectroscopic Redshift for the Cl 0024+16 Multiple Arc System: Implications for the Central Mass Distribution. Astrophys J. 2000 May 1;534(1):L15-L18. PubMed PMID: 10790060.

14: Taylor EN, Stampfer MJ, Curhan GC. Obesity, weight gain, and the risk of kidney stones. JAMA. 2005 Jan 26;293(4):455-62. PubMed PMID: 15671430.