Talabostat mesylate
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MedKoo CAT#: 202730

CAS#: 150080-09-4

Description: Talabostat, also known as PT-100, is dipeptidyl peptidase inhibitor with antineoplastic and hematopoiesis- stimulating activities. By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell- dependent activity. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. Dipeptidyl peptidases are involved in the activation of polypeptide hormones and chemokines.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 750
1g
USD 3250
Size
Price

25mg
USD 250
200mg
USD 1250
2g
USD 4850
Size
Price

50mg
USD 450
500mg
USD 2250
5g
USD 6950

Talabostat mesylate, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 2g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 202730
Name: Talabostat mesylate
CAS#: 150080-09-4
Chemical Formula: C10H23BN2O6S
Exact Mass: 214.15
Molecular Weight: 310.17
Elemental Analysis: C, 50.50; H, 8.95; B, 5.05; N, 13.09; O, 22.42


Related CAS #: 150080-09-4 (mesylate)   149682-77-9 (free base)  

Synonym: PT-100, PT100, PT 100, D05989, Val-boro-pro, Talabostat

IUPAC/Chemical Name: (R)-1-((S)-2-amino-3-methylbutanoyl)pyrrolidin-2-ylboronic acid methanesulfonic acid (1:1)

InChi Key: OXYYOEIGQRXGPI-WSZWBAFRSA-N

InChi Code: InChI=1S/C9H19BN2O3.CH4O3S/c1-6(2)8(11)9(13)12-5-3-4-7(12)10(14)15;1-5(2,3)4/h6-8,14-15H,3-5,11H2,1-2H3;1H3,(H,2,3,4)/t7-,8-;/m0./s1

SMILES Code: OB([C@H]1N(C([C@@H](N)C(C)C)=O)CCC1)O.CS(=O)(O)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the 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, not in water

Shelf Life:
>5 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: Huang Y, Simms AE, Mazur A, Wang S, León NR, Jones B, Aziz N, Kelly T. Fibroblast activation protein-α promotes tumor growth and invasion of breast cancer cells through non-enzymatic functions. Clin Exp Metastasis. 2011 Aug;28(6):567-79. doi: 10.1007/s10585-011-9392-x. Epub 2011 May 22. PubMed PMID: 21604185.

2: Meany H, Balis FM, Aikin A, Whitcomb P, Murphy RF, Steinberg SM, Widemann BC, Fox E. Pediatric phase I trial design using maximum target inhibition as the primary endpoint. J Natl Cancer Inst. 2010 Jun 16;102(12):909-12. Epub 2010 May 11. PubMed PMID: 20460632; PubMed Central PMCID: PMC2886096.

3: Eager RM, Cunningham CC, Senzer NN, Stephenson J Jr, Anthony SP, O'Day SJ, Frenette G, Pavlick AC, Jones B, Uprichard M, Nemunaitis J. Phase II assessment of talabostat and cisplatin in second-line stage IV melanoma. BMC Cancer. 2009 Jul 30;9:263. PubMed PMID: 19643020; PubMed Central PMCID: PMC2731782.

4: Eager RM, Cunningham CC, Senzer N, Richards DA, Raju RN, Jones B, Uprichard M, Nemunaitis J. Phase II trial of talabostat and docetaxel in advanced non-small cell lung cancer. Clin Oncol (R Coll Radiol). 2009 Aug;21(6):464-72. Epub 2009 Jun 5. PubMed PMID: 19501491.

5: Pennisi A, Li X, Ling W, Khan S, Gaddy D, Suva LJ, Barlogie B, Shaughnessy JD, Aziz N, Yaccoby S. Inhibitor of DASH proteases affects expression of adhesion molecules in osteoclasts and reduces myeloma growth and bone disease. Br J Haematol. 2009 Jun;145(6):775-87. Epub 2009 Apr 8. PubMed PMID: 19388929; PubMed Central PMCID: PMC2748971.

6: Cristillo AD, Galmin L, Restrepo S, Hudacik L, Suschak J, Lewis B, Draghia-Akli R, Aziz N, Weiss D, Markham P, Pal R. HIV-1 Env vaccine comprised of electroporated DNA and protein co-administered with Talabostat. Biochem Biophys Res Commun. 2008 May 23;370(1):22-6. Epub 2008 Mar 7. PubMed PMID: 18329382.

7: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Dec;29(10):697-735. PubMed PMID: 18200333.

8: Narra K, Mullins SR, Lee HO, Strzemkowski-Brun B, Magalong K, Christiansen VJ, McKee PA, Egleston B, Cohen SJ, Weiner LM, Meropol NJ, Cheng JD. Phase II trial of single agent Val-boroPro (Talabostat) inhibiting Fibroblast Activation Protein in patients with metastatic colorectal cancer. Cancer Biol Ther. 2007 Nov;6(11):1691-9. Epub 2007 Aug 14. PubMed PMID: 18032930.

9: Cunningham CC. Talabostat. Expert Opin Investig Drugs. 2007 Sep;16(9):1459-65. Review. PubMed PMID: 17714031.

10: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2006 Dec;28(10):719-40. PubMed PMID: 17235418.

11: Molecule of the month. Talabostat. Drug News Perspect. 2006 Jun;19(5):299. PubMed PMID: 16941051.