| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
OTX008's growth inhibitory concentration (GI50) spans from 3 to 500 μM in a variety of human solid tumor cell lines. In the mold group, there was a strong association found between the levels of protein expression and Gal1 mRNA (LGALS1) and OTX008 GI50 values. OTX008 stimulates G2/M cell cycle signaling through CDK1 and suppresses Gal1 expression as well as ERK1/2- and AKT-dependent survival pathways in SQ20B and A2780-1A9 cells. OTX008 inhibits head formation brought on by exogenous Gal1 and strengthens the anti-apoptotic action of semaphorin-3A (Sema3A) in SQ20B cells [1]. OTX008 has an impact on the shortest, motility, proliferation, and umbilical cord of endothelial cells. Additionally, variations in gravity between cell lines (IC50: 1-190 μM) prevent tumor growth [2].
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| ln Vivo |
The growth of subcutaneously transplanted A2780-1A9 tumors is transcribed by OTX008. OTX008 decreases blood vessel density and transcriptionally controls the expression of Gal1, Ki67, and VEGFR2. When OTX008 was initially introduced, it showed promise in terms of jump treatment and cell multiple toxicity [1].
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| References |
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| Additional Infomation |
OTX008 has been used in trials studying the treatment of Solid Tumors.
Galectin-1 Inhibitor OTX008 is a calixarene-based compound and galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. Upon subcutaneous administration, galectin-1 inhibitor OTX008 binds Gal-1 which leads to Gal-1 oxidation and proteasomal degradation, through an as of yet not fully elucidated mechanism, and eventually downregulation of Gal-1. This decreases tumor cell growth and inhibits angiogenesis. Gal-1, a multifunctional carbohydrate-binding protein, is often overexpressed on tumor cells and plays a key role in cancer cell proliferation, apoptosis, tumor angiogenesis and evasion of immune responses. |
| Molecular Formula |
C52H72N8O8
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|---|---|
| Molecular Weight |
937.18
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| Exact Mass |
936.547
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| CAS # |
286936-40-1
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| PubChem CID |
11953346
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
1143.4±65.0 °C at 760 mmHg
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| Flash Point |
645.3±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
4.14
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
68
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| Complexity |
1250
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CQVAQQNDZCZBSU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C52H72N8O8/c1-57(2)25-21-53-45(61)33-65-49-37-13-9-14-38(49)30-40-16-11-18-42(51(40)67-35-47(63)55-23-27-59(5)6)32-44-20-12-19-43(52(44)68-36-48(64)56-24-28-60(7)8)31-41-17-10-15-39(29-37)50(41)66-34-46(62)54-22-26-58(3)4/h9-20H,21-36H2,1-8H3,(H,53,61)(H,54,62)(H,55,63)(H,56,64)
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| Chemical Name |
N-[2-(dimethylamino)ethyl]-2-[[26,27,28-tris[2-[2-(dimethylamino)ethylamino]-2-oxoethoxy]-25-pentacyclo[19.3.1.13,7.19,13.115,19]octacosa-1(25),3(28),4,6,9(27),10,12,15,17,19(26),21,23-dodecaenyl]oxy]acetamide
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| Synonyms |
OTX008; OTX 008; OTX-008
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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) |
Ethanol : ~33.33 mg/mL (~35.56 mM)
DMSO : ~5 mg/mL (~5.34 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.33 mM) (saturation unknown) in 10% EtOH + 90% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (0.53 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 5.0 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. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (0.53 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. Solubility in Formulation 4: ≥ 0.5 mg/mL (0.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 5: 0.5 mg/mL (0.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0670 mL | 5.3352 mL | 10.6703 mL | |
| 5 mM | 0.2134 mL | 1.0670 mL | 2.1341 mL | |
| 10 mM | 0.1067 mL | 0.5335 mL | 1.0670 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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