BMS-833923
Based on 1 Customer Validation
BMS-833923 (XL-139) is an orally biocompatible Smoothened (Smo) inhibitor with anti-tumor activity. It can inhibit the binding of BODIPY cyclopamine to SMO in a dose-dependent manner with an IC50 of 21 nM.
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- Pureté: 99.82%
- CAS No.: 1059734-66-5
- Formule: C30H27N5O
- Masse moléculaire:473.57
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
BMS‐833923 inhibits the expression of downstream effectors in the HH pathway (GLI1 and PTCH1) wild‐type SMO and activated mutant forms of SMO expressing cells (IC50: 6-35 nM)[1].
BMS‐833923 (2.5-10 μM, 48 h) inhibits cell proliferation of both A549 and H1299 cells[2].
BMS‐833923 (3 µM) inhibits osteoblast differentiation and mineralization of hMSCs, determined by decreased ALP activity and downregulation of osteoblast-related gene expression[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human MSCs
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Concentration:3 µM
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Incubation Time:48 h
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Result:Inhibited gene expression of ALP, ON, COL1A1, GLI1, and PTCH1.
BMS-833923 (30 mg/kg, p.o., seven consecutive days) alone or together with Gemcitabine (HY-17026) (40 mg/kg, i.p., at the 1st, 4th and 7th day) reduces tumor volume (to 60% and 32% respectively) in a nu/nu mice xenograft model of cholangiocarcinoma[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1059734-66-5
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Appearance Solid
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Masse moléculaire 473.57
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Formule C30H27N5O
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC(CNC)=CC=C1C)C2=CC=C(NC3=NC(C4=CC=CC=C4)=C5C=CC=CC5=N3)C=C2
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Synonyms
XL-139
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 50 mg/mL (105.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[2]. Du J, et al. Disruption of SHH signaling cascade by SBE attenuates lung cancer progression and sensitizes DDP treatment. Sci Rep. 2017 May 15;7(1):1899. [Content Brief]
[3]. AlMuraikhi N, et al. Hedgehog Signaling Inhibition by Smoothened Antagonist BMS-833923 Reduces Osteoblast Differentiation and Ectopic Bone Formation of Human Skeletal (Mesenchymal) Stem Cells. Stem Cells Int. 2019 Nov 21;2019:3435901. [Content Brief]
[4]. Gu D, et al. Simultaneous Inhibition of MEK and Hh Signaling Reduces Pancreatic Cancer Metastasis. Cancers (Basel). 2018 Oct 26;10(11):403. [Content Brief]
[5]. Riedlinger D, et al. Hedgehog pathway as a potential treatment target in human cholangiocarcinoma. J Hepatobiliary Pancreat Sci. 2014 Aug;21(8):607-15. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1116 mL | 10.5581 mL | 21.1162 mL | 52.7905 mL |
| 5 mM | 0.4223 mL | 2.1116 mL | 4.2232 mL | 10.5581 mL | |
| 10 mM | 0.2112 mL | 1.0558 mL | 2.1116 mL | 5.2791 mL | |
| 15 mM | 0.1408 mL | 0.7039 mL | 1.4077 mL | 3.5194 mL | |
| 20 mM | 0.1056 mL | 0.5279 mL | 1.0558 mL | 2.6395 mL | |
| 25 mM | 0.0845 mL | 0.4223 mL | 0.8446 mL | 2.1116 mL | |
| 30 mM | 0.0704 mL | 0.3519 mL | 0.7039 mL | 1.7597 mL | |
| 40 mM | 0.0528 mL | 0.2640 mL | 0.5279 mL | 1.3198 mL | |
| 50 mM | 0.0422 mL | 0.2112 mL | 0.4223 mL | 1.0558 mL | |
| 60 mM | 0.0352 mL | 0.1760 mL | 0.3519 mL | 0.8798 mL | |
| 80 mM | 0.0264 mL | 0.1320 mL | 0.2640 mL | 0.6599 mL | |
| 100 mM | 0.0211 mL | 0.1056 mL | 0.2112 mL | 0.5279 mL |
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