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2mg |
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5mg |
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10mg |
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25mg |
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100mg |
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Purity: ≥98%
Taladegib (formerly LY2940680, LY 2940680, LY-2940680) is a potent and orally bioavailable Hedgehog pathway antagonist of the smoothened receptor being developed by Eli Lilly for the treatment of cancer. It blocks the Hedgehog (Hh) signaling pathway by attaching to the Smoothened (Smo) receptor. Taladegib possesses the potential to be applied to cancer patients who are vismodegib-resistant..
Targets |
Smoothened
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ln Vivo |
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Animal Protocol |
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References |
Molecular Formula |
C26H24F4N6O
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Molecular Weight |
512.5
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Exact Mass |
512.19
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Elemental Analysis |
C, 60.93; H, 4.72; F, 14.83; N, 16.40; O, 3.12
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CAS # |
1258861-20-9
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Related CAS # |
1258861-20-9; 1258861-21-0 (HCl)
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Appearance |
White solid powder
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SMILES |
CN1C(=CC=N1)C2=NN=C(C3=CC=CC=C32)N4CCC(CC4)N(C)C(=O)C5=C(C=C(C=C5)F)C(F)(F)F
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InChi Key |
SZBGQDXLNMELTB-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C26H24F4N6O/c1-34(25(37)20-8-7-16(27)15-21(20)26(28,29)30)17-10-13-36(14-11-17)24-19-6-4-3-5-18(19)23(32-33-24)22-9-12-31-35(22)2/h3-9,12,15,17H,10-11,13-14H2,1-2H3
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Chemical Name |
4-fluoro-N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoromethyl)benzamide
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.88 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 (4.88 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 (4.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9512 mL | 9.7561 mL | 19.5122 mL | |
5 mM | 0.3902 mL | 1.9512 mL | 3.9024 mL | |
10 mM | 0.1951 mL | 0.9756 mL | 1.9512 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 |
NCT05199584 | Active Recruiting |
Drug: ENV-101 (taladegib) |
Solid Tumors With PTCH1 Loss-of-function Mutations |
Endeavor Biomedicines, Inc. | May 24, 2022 | Phase 2 |
NCT04968574 | Active Recruiting |
Drug: taladegib Drug: placebo |
Idiopathic Pulmonary Fibrosis | Endeavor Biomedicines, Inc. | August 26, 2021 | Phase 2 |
NCT05817240 | Completed | Drug: taladegib Drug: nintedanib |
Idiopathic Pulmonary Fibrosis | Endeavor Biomedicines, Inc. | May 3, 2023 | Phase 1 |
NCT01226485 | Completed | Drug: Taladegib | Advanced Cancer | Eli Lilly and Company | September 2010 | Phase 1 |
NCT02784795 | Completed | Drug: Taladegib Drug: Abemaciclib |
Solid Tumor Breast Cancer |
Eli Lilly and Company | November 4, 2016 | Phase 1 |
Effect of Sonic Hedgehog (Hg) pathway inhibitors on proliferation and apoptosis of mucin and mixed CCA primary cultures.PLoS One.2015 Nov 16;10(11):e0142124. th> |
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