I-BET567
Based on 1 Customer Validation
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.
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- Pureté: 99.49%
- CAS No.: 1887237-54-8
- Formule: C17H18ClN5O2
- Masse moléculaire:359.81
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Epigenetics Compound Library
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Activité biologique
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BRD4 (BD1) 6.9 (pIC50) |
BRD2 7.2 (pIC50) |
I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) effectively inhibites the proliferation of human NMC cell line 11060 in vitro with a mean gpIC50 6.2 (0.63 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NMC line 11060 cells
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Concentration:1.5 nM-30 μM
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Incubation Time:72 hours
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Result:Significantly reduced cell growth.
Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle doga[1].
| species | dose ivb/poc (mg/kg) | CLb (mL/min/kg) | CLb,u (mL/min/kg) | CLrenal (mL/min/kg) | Vss (L/kg) | Vss,u (L/kg) | t1/2 (h) | Fpo (%) | fub |
| rat | 1.3/3 | 25 | 109 | 7 | 2.4 | 10.4 | 1.6 | 99d | 0.23 |
| dog | 1.0/3 | 8.1 | 20 | 6.9 | 1.2 | 2.9 | 1.8 | 98 | 0.41 |
a: Values are mean, n=3 unless otherwise stated. b: IV dose 1h infusion in DMSO and (10%, w/v) Kleptose HPB in saline (2%: 98% (v/v)). c: PO dose vehicle: 1%(w/v) methycellulose (400 cps) (aq). d: Mean n = 2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells) [1]
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Dosage:3, 10, and 30 mg/kg
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Administration:p.o. (once daily for 20 days
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Result:Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg.
Chemical Information
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CAS No. 1887237-54-8
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Appearance Solid
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Masse moléculaire 359.81
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Formule C17H18ClN5O2
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Color White to off-white
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SMILES
O=C(C1=CC2=C(N(C(C)=O)[C@@H](C)C[C@H]2NC3=NC=C(Cl)C=N3)C=C1)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
DMSO : 100 mg/mL (277.92 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (6.95 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.95 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7792 mL | 13.8962 mL | 27.7924 mL | 69.4811 mL |
| 5 mM | 0.5558 mL | 2.7792 mL | 5.5585 mL | 13.8962 mL | |
| 10 mM | 0.2779 mL | 1.3896 mL | 2.7792 mL | 6.9481 mL | |
| 15 mM | 0.1853 mL | 0.9264 mL | 1.8528 mL | 4.6321 mL | |
| 20 mM | 0.1390 mL | 0.6948 mL | 1.3896 mL | 3.4741 mL | |
| 25 mM | 0.1112 mL | 0.5558 mL | 1.1117 mL | 2.7792 mL | |
| 30 mM | 0.0926 mL | 0.4632 mL | 0.9264 mL | 2.3160 mL | |
| 40 mM | 0.0695 mL | 0.3474 mL | 0.6948 mL | 1.7370 mL | |
| 50 mM | 0.0556 mL | 0.2779 mL | 0.5558 mL | 1.3896 mL | |
| 60 mM | 0.0463 mL | 0.2316 mL | 0.4632 mL | 1.1580 mL | |
| 80 mM | 0.0347 mL | 0.1737 mL | 0.3474 mL | 0.8685 mL | |
| 100 mM | 0.0278 mL | 0.1390 mL | 0.2779 mL | 0.6948 mL |
I-BET567 Related Classifications
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