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| ln Vitro |
In addition to acting to reverse drug resistance induced by wild-type BCRP (BCRPR482) and to increase drug uptake and retention, biicodar has efficacy against P-glycoprotein (Pgp) and MRP-1. Bilicoda boosted mitoxantrone and daunorubicin absorption by 55% and 100%, respectively, retention rates by 100% and 60%, and cytotoxicity by 3.1-fold in 8226/Dox6 cells (Pgp). and 6.9 instances. In HL60/Adr (MRP-1) and 8226/MR20 cells (BCRP(R482)), biicodar likewise improves uptake, retention, and cytotoxicity; however, it has no effect on MCF7 AdVP3000 cells (BCRP(R482T)) [1]. A non-macrocyclic derivative of pipecolate, VX-710 interacts to the FK506 receptor protein. It has been demonstrated that VX-710 can regain sensitivity to a variety of multidrug-resistant cells, such as those found in leukemia, cancer, melanoma, and myeloma [2]. With EC50 values of 0.75 and 0.55 μM, respectively, bisicodar may efficiently block the photoaffinity labeling of P-glycoprotein by [3H]azidopine or [125I]iodoaryl azido-prazosin [3].
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| References |
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| Additional Infomation |
Biricodar is an alpha-amino acid ester.
The pipecolinate derivative biricodar (VX-710) is a clinically applicable modulator of P-glycoprotein (Pgp) and multidrug resistance protein (MRP-1). Biricodar is a pipecolinate derivative. Functioning as a modulator of P-glycoprotein (P-gp) and multidrug resistance protein (MRP-1), biricodar restores drug sensitivity to cells expressing P-glycoprotein and MRP1, the cellular efflux pumps that are the major causes in tumor cell resistance to chemotherapeutic agents. This agent binds directly to Pgp and MRP-1 and inhibits efflux pump activity, resulting in increased intracellular accumulation and retention of cytotoxic agents. Drug Indication Administered intravenously, biricodar dicitrate is to be used in combination with cancer chemotherapy agents. Mechanism of Action Vertex’s research shows that biricodar dicitrate can enhance the accumulation of chemotherapy agents in tumor cells by blocking the drug pumps P-gp and MRP, and that it is capable of restoring the sensitivity of tumors to treatment with chemotherapeutic agents. |
| Molecular Formula |
C34H41N3O7
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|---|---|
| Molecular Weight |
603.71
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| Exact Mass |
603.294
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| CAS # |
159997-94-1
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| PubChem CID |
3037617
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| Appearance |
Colorless to light yellow ointment
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| Density |
1.195g/cm3
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| Boiling Point |
752.1ºC at 760 mmHg
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| Flash Point |
408.7ºC
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| Vapour Pressure |
1.66E-22mmHg at 25°C
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| Index of Refraction |
1.565
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| LogP |
4.961
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
44
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| Complexity |
866
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C([C@]1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1C(C(C1C([H])=C(C(=C(C=1[H])OC([H])([H])[H])OC([H])([H])[H])OC([H])([H])[H])=O)=O)=O)C([H])(C([H])([H])C([H])([H])C([H])([H])C1=C([H])N=C([H])C([H])=C1[H])C([H])([H])C([H])([H])C([H])([H])C1=C([H])N=C([H])C([H])=C1[H]
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| InChi Key |
CGVWPQOFHSAKRR-NDEPHWFRSA-N
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| InChi Code |
InChI=1S/C34H41N3O7/c1-41-29-20-26(21-30(42-2)32(29)43-3)31(38)33(39)37-19-5-4-16-28(37)34(40)44-27(14-6-10-24-12-8-17-35-22-24)15-7-11-25-13-9-18-36-23-25/h8-9,12-13,17-18,20-23,27-28H,4-7,10-11,14-16,19H2,1-3H3/t28-/m0/s1
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| Chemical Name |
1,7-Dipyridin-3-ylheptan-4-yl (2S)-1-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate
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| Synonyms |
Biricodar Incel VX710VX-710 VX 710
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.6564 mL | 8.2821 mL | 16.5642 mL | |
| 5 mM | 0.3313 mL | 1.6564 mL | 3.3128 mL | |
| 10 mM | 0.1656 mL | 0.8282 mL | 1.6564 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 |
| NCT00003847 | TERMINATED | Drug: biricodar dicitrate Drug: doxorubicin hydrochloride Drug: vincristine sulfate |
Lung Cancer | Vertex Pharmaceuticals Incorporated | 1998-12 | Phase 2 |
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