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Talabostat (PT-100; PT100 Val-boroPro) is a novel, orally available and potent inhibitor of multiple dipeptidyl peptidase such as DPP4, DPP8, and DPP9 (Ki = 0.18 nM) with anticancer and hematopoiesis-stimulating activities. It inhibits AML progression in vivo and induces lytic cell death in sensitive AML cell lines.
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| ln Vitro |
Talabostat (Val-boroPro) inhibits dipeptidyl peptidases, like FAP, by cleaving the N-terminal Xaa-Pro or Xaa-Ala residues. This stimulates the synthesis of cytokines and chemokines, as well as specific T-cell immunity and T-cell reliant activity[3]. Talabostat (Val-boroPro) interacts with the catalytic region with high affinity and competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV[4].
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| ln Vivo |
Both the innate and adaptive immune systems' tumor-fighting capabilities can be enhanced by talabostat (Val-boroPro; PT100). Talabostat (Val-boroPro), in the WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, induces tumor regression and rejection. It seems that protective immune memory and tumor-specific CTL are involved in the anticancer impact. Treatment with talabostat (Val-boroPro) increases the mRNA expression of cytokines and chemokines in WEHI 164-inoculated mice, which are known to facilitate T-cell priming and chemoattraction of T cells and innate effector cells[4].
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| References |
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| Additional Infomation |
Talabostat is a small molecule 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.
See also: Talabostat Mesylate (annotation moved to). Drug Indication Investigated for use/treatment in lymphoma (non-hodgkin's), leukemia (lymphoid), lung cancer, melanoma, and pancreatic cancer. |
| Molecular Formula |
C9H19BN2O3
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|---|---|
| Molecular Weight |
214.07
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| Exact Mass |
214.148
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| CAS # |
149682-77-9
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| Related CAS # |
Talabostat mesylate;150080-09-4;Talabostat isomer mesylate
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| PubChem CID |
6918572
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
421.4±55.0 °C at 760 mmHg
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| Flash Point |
208.7±31.5 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.514
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| LogP |
0.01
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
15
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| Complexity |
235
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)[C@H](N)C(N1[C@H](B(O)O)CCC1)=O
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| InChi Key |
FKCMADOPPWWGNZ-YUMQZZPRSA-N
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| 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
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| Chemical Name |
((R)-1-(L-Valyl)pyrrolidin-2-yl)boronic acid
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| Synonyms |
PT100 Val-boroPro PT-100 Talabostat
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 40 mg/mL (~186.85 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6714 mL | 23.3568 mL | 46.7137 mL | |
| 5 mM | 0.9343 mL | 4.6714 mL | 9.3427 mL | |
| 10 mM | 0.4671 mL | 2.3357 mL | 4.6714 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.
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