| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Description: Talabostat mesylate, the mesylate salt of Talabostat (PT-100; PT100 Val-boroPro), is an orally available inhibitor of dipeptidyl peptidase (DPP4, DPP8, and DPP9) with a Ki of 0.18 nM. It has hematopoiesis-stimulating and anticancer properties.
| Targets |
DPP-4
|
|---|---|
| ln Vitro |
Talabostat mesylate (Val-boroPro mesylate) inhibits dipeptidyl peptidases, like FAP, by cleaving N-terminal Xaa-Pro or Xaa-Ala residues. This leads to the stimulation of cytokine and chemokine production, as well as specific T-cell immunity and T-cell dependent activity[3].
Talabostat mesylate (Val-boroPro mesylate) interacts with the catalytic site with high affinity and competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV[4]. |
| ln Vivo |
Talabostat mesylate (Val-boroPro mesylate) can elicit immune responses from the innate and adaptive branches of the immune system against tumors.
Talabostat mesylate, also known as Val-boroPro mesylate, induces tumor regression and rejection in the WEHI 164 fibrosarcoma, EL4, and A20/2J lymphoma models. Tumor-specific CTL and memory immunity seem to play a role in the antitumor effect. Talabostat mesylate (Val-boroPro mesylate) treatment of the WEHI 164-inoculated mice results in an increase in the mRNA expression of cytokines and chemokines that are known to support T-cell priming and innate effector cell and T cell chemoattraction[4]. |
| Animal Protocol |
Mice: BLM (0.5mg/kg/day) is injected into male mice's nostrils on days -7, -6, -5, -2, -1, and 0. From day 1 to day 14, talabostat (40 µg/mouse) or vehicle (0.9% NaCl) is dosed twice a day. MRIs are done on days 0, 7, and 14 as well as prior to BLM. The animals are put to sleep after the final MRI scan, and their lungs are taken out for histology and quantitative real-time polymerase chain reaction (qRT-PCR) analysis[4].
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| References |
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| Molecular Formula |
C10H23BN2O6S
|
|---|---|
| Molecular Weight |
310.17
|
| Exact Mass |
214.15
|
| Elemental Analysis |
C, 50.50; H, 8.95; B, 5.05; N, 13.09; O, 22.42
|
| CAS # |
150080-09-4
|
| Related CAS # |
Talabostat isomer mesylate;Talabostat;149682-77-9
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| Appearance |
Solid powder
|
| SMILES |
B([C@@H]1CCCN1C(=O)[C@H](C(C)C)N)(O)O.CS(=O)(=O)O
|
| 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
|
| Chemical Name |
[(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid;methanesulfonic acid
|
| Synonyms |
Talabostat; BXCL701; BXCL-701; BXCL 701; Val-boro-pro; PT-100; PT100, PT 100; D05989
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O: ~250 mg/mL (~806 mM)
DMSO: ≥ 40 mg/mL (~129 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (322.39 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 5: 50 mg/mL (161.20 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2240 mL | 16.1202 mL | 32.2404 mL | |
| 5 mM | 0.6448 mL | 3.2240 mL | 6.4481 mL | |
| 10 mM | 0.3224 mL | 1.6120 mL | 3.2240 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04171219 | Active Recruiting |
Biological: Pembrolizumab Drug: Talabostat Mesylate |
Advanced Malignant Solid Neoplasm Recurrent Malignant Solid Neoplasm |
M.D. Anderson Cancer Center | March 19, 2020 | Phase 2 |
| NCT00303940 | Completed | Drug: carboplatin Drug: talabostat mesylate |
Kidney Cancer Liver Cancer |
National Institutes of Health Clinical Center (CC) |
December 2005 | Phase 1 |
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