BGB-8035
Based on 1 Customer Validation
BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.00%
- CAS 番号: 2283349-24-4
- 分子式: C24H31N5O4
- 分子量:453.53
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
IC50: 1.1 nM (BTK), 99 nM (TEC), and 621 nM (EGFR)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: (S)-20a; BGB-8035
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Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
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[PMID: 36912866] |
| Ramos | IC50 |
>10 μM
Compound: (S)-20a; BGB-8035
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Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
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[PMID: 36912866] |
| Rec1 | IC50 |
10.4 nM
Compound: (S)-20a; BGB-8035
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Antiproliferative activity against human REC1 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human REC1 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo luminescent cell viability assay
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[PMID: 36912866] |
BGB-8035 is nontoxicin HEK293 and Ramos cells (IC50 > 10 μM, both)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BGB-8035 (1, 3, 10, 30 mg/kg; PO; BID; 13 days) inhibits arthritis as measured by clinical scores in a dose-dependent manner in the Lewis rats aged 8-9 weeks with CIA model and prevents the CIA model-associated body weight loss[1].
Pharmacokinetic Parameters of BGB-8035 in Rats and Dogs[1].
| Rats (IV; 1 mg/kg) | Rats (PO; 5 mg/kg) | Dogs (IV; 1 mg/kg) | Dogs (PO; 2.5 mg/kg) | |
| T1/2 (h) | 1.0 | 2.5 | ||
| CL (mL/min/kg) | 24.4 | 6.89 | ||
| Vss (L/kg) | 0.9 | 0.74 | ||
| Tmax (h) | 0.25 | 0.42 | ||
| Cmax (ng/mL) | 667 | 1246 | ||
| AUCinf (h∗ng/mL) | 964 | 2645 | ||
| F (%) | 26.4 | 43 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NOD/SCID mice at 9 weeks of age with REC-1 MCL xenografts[1]
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Dosage:7.5, 15, 30 mg/kg
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Administration:PO; BID; 16 days
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Result:Demonstrated dose-dependent antitumor activity, with TGI values of 64.1, 73.6, and 79.9%, respectively.
化学情報
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CAS 番号 2283349-24-4
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性状 Solid
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分子量 453.53
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分子式 C24H31N5O4
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Color White to off-white
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SMILES
C=CC(N1CCC(CC1)[C@@H]2CCNC3=C(C(C4=CC(OC)=C(C(OC)=C4)C)=NN32)C(N)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (110.25 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 90% (20% SBE-β-CD in Saline)
Solubility: 1.25 mg/mL (2.76 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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.
純度とドキュメンテーション
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データシート (279 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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取扱説明書 (2659 KB)
参考文献
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. 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 | 2.2049 mL | 11.0246 mL | 22.0493 mL | 55.1231 mL |
| 5 mM | 0.4410 mL | 2.2049 mL | 4.4099 mL | 11.0246 mL | |
| 10 mM | 0.2205 mL | 1.1025 mL | 2.2049 mL | 5.5123 mL | |
| 15 mM | 0.1470 mL | 0.7350 mL | 1.4700 mL | 3.6749 mL | |
| 20 mM | 0.1102 mL | 0.5512 mL | 1.1025 mL | 2.7562 mL | |
| 25 mM | 0.0882 mL | 0.4410 mL | 0.8820 mL | 2.2049 mL | |
| 30 mM | 0.0735 mL | 0.3675 mL | 0.7350 mL | 1.8374 mL | |
| 40 mM | 0.0551 mL | 0.2756 mL | 0.5512 mL | 1.3781 mL | |
| 50 mM | 0.0441 mL | 0.2205 mL | 0.4410 mL | 1.1025 mL | |
| 60 mM | 0.0367 mL | 0.1837 mL | 0.3675 mL | 0.9187 mL | |
| 80 mM | 0.0276 mL | 0.1378 mL | 0.2756 mL | 0.6890 mL | |
| 100 mM | 0.0220 mL | 0.1102 mL | 0.2205 mL | 0.5512 mL |
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