Talabostat

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MedKoo CAT#: 564721

CAS#: 149682-77-9 (free base)

Description: Talabostat, also known as PT-100 and BXCL701, 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.

Chemical Structure

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Talabostat
CAS# 149682-77-9 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 564721
Name: Talabostat
CAS#: 149682-77-9 (free base)
Chemical Formula: C9H19BN2O3
Exact Mass: 214.15
Molecular Weight: 214.070
Elemental Analysis: C, 50.50; H, 8.95; B, 5.05; N, 13.09; O, 22.42

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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

Synonym: BXCL701; BXCL 701; BXCL-701; PT-100, PT100, PT 100, D05989, Val-boroPro; Talabostat

IUPAC/Chemical Name: ((R)-1-(L-Valyl)pyrrolidin-2-yl)boronic acid

InChi Key: FKCMADOPPWWGNZ-YUMQZZPRSA-N

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

SMILES Code: N[C@@H](C(C)C)C(N1[C@H](B(O)O)CCC1)=O

Appearance: Solid powder

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

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: >3 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).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 214.07 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: 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. doi: 10.1186/1471-2407-9-263. PubMed PMID: 19643020; PubMed Central PMCID: PMC2731782.

2: 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. doi: 10.1016/j.clon.2009.04.007. Epub 2009 Jun 5. PubMed PMID: 19501491.

3: 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. doi: 10.1016/j.bbrc.2008.02.145. Epub 2008 Mar 7. PubMed PMID: 18329382.

4: 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.

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

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