Motixafortide
Based on 3 publication(s) in Google Scholar
Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM.
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- 純度: 99.76%
- CAS 番号: 664334-36-5
- 分子式: C97H144FN33O19S2
- 分子量:2159.52
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Motixafortide
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生物活性
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CXCR4 ~1 nM (IC50) |
Motixafortide (BKT140) displays selective toxicity toward AmL and MM cells. Treatment with Motixafortide (BKT140) can overcome IL-6 dependent proliferation and survival of ARH77 MM cells. Motixafortide (BKT140) specifically triggers CXCR4-dependent cell death in leukemia and MM cells. Motixafortide (BKT140) stimulates apoptotic cell death in leukemia and MM cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 664334-36-5
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性状 Solid
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分子量 2159.52
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分子式 C97H144FN33O19S2
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Color White to off-white
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別名
BKT140 (4-fluorobenzoyl); BL-8040; TF14016
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配列
{4-Fluorobenzoyl}-Arg-Arg-{2-Naph-Ala}-Cys-Tyr-{Cit}-Lys-{d-Lys}-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2 (Disulfide bridge: Cys4-Cys13)
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シーケンスの短縮
{4-Fluorobenzoyl}-RR-{2-Naph-Ala}-CY-{Cit}-K-{d-Lys}-PYR-{Cit}-CR-NH2 (Disulfide bridge: Cys4-Cys13)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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J Transl Med
CXCL12/CXCR4 axis mediates CD8 + T cell overactivation in the progression of viral myocarditis. [Abstract]2025 Apr 4;23(1):399. PMID: 40186195 -
Sci Rep
C-terminal-modified LY2510924: a versatile scaffold for targeting C-X-C chemokine receptor type 4. [Abstract]2019 Oct 25;9(1):15284. PMID: 31653903 -
溶剤 & 溶解度
DMSO : 100 mg/mL (46.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (23.15 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 110 mg/mL (50.94 mM); Clear solution; Need ultrasonic
プロトコル
Hematopoietic cancer cells are incubated with different concentrations of Motixafortide (BKT140) or AMD3100 for 24 hours. Motixafortide (BKT140) is treated with 1M hydrochloric acid (HCL) to achieve a pH of 2.7 to 3 at room temperature for 30 minutes and the pH is adjusted to 7 using concentrated NaOH. Proteinase K is added to Motixafortide (BKT140) at a final concentration of 100 mg/mL, incubated at 37°C for 1 hour, and inactivated by heat treatment (65°C for 30 minutes). After incubation, cells are stained with propidium iodide and the percent of viable PI-negative cells in culture is determined[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Severe combined immune-deficient (SCID)/beige mice (C.B-17/IcrHsd-SCID-bg) are used in the study. NB4 cells resuspended in PBS are injected subcutaneously into the flanks of the mice (200 μL per mouse containing 5×106 cells). Tumor growth is monitored daily, and mice are randomized to drug-treated or control PBS-treated groups (10 mice per group) when the tumor size (width×length) reaches 0.04 cm2. BKT140 is administered subcutaneously at a dose of 200 μg per mouse each day for 5 days[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Peled A, et al. The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cellsin patients with multiple myeloma. Clin Cancer Res. 2014 Jan 15;20(2):469-79. [Content Brief]
[2]. Beider K, et al. CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth. Exp Hematol. 2011 Mar;39(3):282-92. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.4631 mL | 2.3153 mL | 4.6307 mL | 11.5766 mL |
| 5 mM | 0.0926 mL | 0.4631 mL | 0.9261 mL | 2.3153 mL | |
| 10 mM | 0.0463 mL | 0.2315 mL | 0.4631 mL | 1.1577 mL | |
| 15 mM | 0.0309 mL | 0.1544 mL | 0.3087 mL | 0.7718 mL | |
| 20 mM | 0.0232 mL | 0.1158 mL | 0.2315 mL | 0.5788 mL | |
| DMSO | 25 mM | 0.0185 mL | 0.0926 mL | 0.1852 mL | 0.4631 mL |
| 30 mM | 0.0154 mL | 0.0772 mL | 0.1544 mL | 0.3859 mL | |
| 40 mM | 0.0116 mL | 0.0579 mL | 0.1158 mL | 0.2894 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Motixafortide 関連分類
HY-P0171 関連分類
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