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5mg |
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10mg |
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25mg |
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50mg |
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Balixafortide (POL-6326), a synthetic cyclopeptide derived from polyphemusin, is a novel, potent and orally bioavailable inhibitor of CXC chemokine receptor 4 (CXCR4, IC 50=10 nM) with anticancer activity. CXCR4 is a member of the G-coupled protein receptor (GPCR) transmembrane receptor class.
Targets |
CXCR4 ( IC50 < 10 nM )
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ln Vitro |
Benaxafortide significantly reduces pERK/pAKT signaling in the lymphoma lines Jurkat (IC50 < 400 nM) and Namalwa (IC50 < 200 nM). In MDA MB 231 breast cancer cells (IC50 < 20 nM), Namalwa and Jurkat cells (IC50 < 10 nM), benaxafortide effectively inhibits SDF-1 dependent chemotaxis (Table 1)[1].
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ln Vivo |
Balixafortide has been optimized with balanced plasma protein binding, increased plasma and microsomal stability, and favorable mouse absorption, distribution, metabolism, and excretion (ADME) properties in mind[1].
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Animal Protocol |
C57BL/6NCrl wild-type (WT) mice, domestic (DanBred hybrid) female pigs
8 mg/kg, 3 mg/kg IV |
References |
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Molecular Formula |
C84H118N24O21S2
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Molecular Weight |
1864.1
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Exact Mass |
1862.83
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Elemental Analysis |
C, 49.00; H, 5.53; F, 7.75; N, 15.24; O, 19.58; S, 2.91
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CAS # |
1051366-32-5
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Related CAS # |
Balixafortide TFA; 1051366-32-5
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Appearance |
Solid powder
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SMILES |
C[C@H]1C(=O)N[C@H]2CSSC[C@@H](C(=O)N[C@H](C(=O)C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H]3CCCN3C(=O)[C@@H](NC(=O)[C@@H](NC2=O)CO)C)CCN)CCCNC(=N)N)CC4=CC=C(C=C4)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H]5CCCN5C(=O)[C@@H]6CCCN6C(=O)[C@@H](NC(=O)[C@@H](NN1)CC7=CN=CN7)CC8=CC=C(C=C8)O)CCCCN)CCC(=O)N)CC9=CC=C(C=C9)O
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InChi Key |
OYWQJZAVFWOOBF-WBMPNIIXSA-N
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InChi Code |
InChI=1S/C84H118N24O21S2/c1-44-70(116)102-62-41-130-131-42-63(77(123)98-57(35-46-14-20-50(110)21-15-46)69(115)68(114)53(10-5-31-91-84(88)89)94-73(119)56(28-30-86)97-79(125)64-11-6-32-106(64)81(127)45(2)93-76(122)61(40-109)101-78(62)124)103-74(120)58(36-47-16-22-51(111)23-17-47)99-72(118)55(26-27-67(87)113)95-71(117)54(9-3-4-29-85)96-80(126)65-12-7-33-107(65)83(129)66-13-8-34-108(66)82(128)60(37-48-18-24-52(112)25-19-48)100-75(121)59(105-104-44)38-49-39-90-43-92-49/h14-25,39,43-45,53-66,104-105,109-112H,3-13,26-38,40-42,85-86H2,1-2H3,(H2,87,113)(H,90,92)(H,93,122)(H,94,119)(H,95,117)(H,96,126)(H,97,125)(H,98,123)(H,99,118)(H,100,121)(H,101,124)(H,102,116)(H,103,120)(H4,88,89,91)/t44-,45-,53-,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64+,65+,66-/m0/s1
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Chemical Name |
3-[(1R,4S,7S,10S,16S,22R,25S,28S,31S,34R,37S,40S,43S,46R,52S,55S)-25-(4-aminobutyl)-43-(2-aminoethyl)-40-(3-carbamimidamidopropyl)-55-(hydroxymethyl)-10,31,37-tris[(4-hydroxyphenyl)methyl]-7-(1H-imidazol-5-ylmethyl)-4,52-dimethyl-3,8,11,17,23,26,29,32,35,38,39,42,45,51,54,57-hexadecaoxo-59,60-dithia-2,5,6,9,12,18,24,27,30,33,36,41,44,50,53,56-hexadecazapentacyclo[32.23.4.012,16.018,22.046,50]henhexacontan-28-yl]propanamide
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Synonyms |
Balixafortide; POL 6326; POL6326; POL6326
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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) |
Water: ~100 mg/mL
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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 | 0.5365 mL | 2.6823 mL | 5.3645 mL | |
5 mM | 0.1073 mL | 0.5365 mL | 1.0729 mL | |
10 mM | 0.0536 mL | 0.2682 mL | 0.5365 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 |
NCT01837095 | Completed | Drug: POL6326 | Metastatic Breast Cancer | Polyphor Ltd. | June 2013 | Phase 1 |
NCT01841476 | Recruiting | Drug: POL6326 | Healthy | Polyphor Ltd. | February 2012 | Phase 1 |
NCT01105403 | Completed | Drug: POL6326 | Multiple Myeloma | Polyphor Ltd. | April 2009 | Phase 2 |
NCT01413568 | Completed | Drug: POL6326 Procedure: Leukapheresis |
Myeloproliferative Disorders Multiple Myeloma (MM) |
Polyphor Ltd. | April 2012 | Phase 1 Phase 2 |
Pharmacodynamics: mobilization of mature hematopoietic cells. a Balixafortide induces dose-dependent leukocytosis with the same kinetics as observed for CD34+ cells (n = 3–6, mean ± SEM); -fold difference between mature cell mobilization with balixafortide and G-CSF was equivalent to that for CD34+ cells. J Transl Med . 2017 Jan 3;15(1):2. td> |