(DHQD)2PHAL
Based on 1 Customer Validation
(DHQD)2PHAL (C-61) is a SYK tyrosine kinase inhibitor. (DHQD)2PHAL blocks SYK-dependent STAT3 signaling and prevents oxidative stress-induced STAT3 tyrosine phosphorylation and DNA-binding activity. (DHQD)2PHAL promotes oxidative stress-induced apoptosis. (DHQD)2PHAL can be used in research on B-cell precursor leukemia and B-lineage acute lymphoblastic leukemia.
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 : 98.0%
- CAS 番号: 140853-10-7
- 分子式: C48H54N6O4
- 分子量:778.98
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保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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
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HY-W002502
(DHQ)2PHALBiochemical Assay Reagent -
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(R)-(+)-2,2-Dimethyl-1,3-dioxolane-4-carboxaldehydeStarting Material
生物活性
製品説明
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Syk |
STAT3 |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAMOS Burkitt’s leukemia/lymphoma cells and BCL-1 cells
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Concentration:1, 10, 50, 100 nM
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Incubation Time:30 min (RAMOS); 1, 5, 10 min (BCL-1)
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Result:Prevented PV-induced and H2O2-induced Y-phosphorylation of SYK in RAMOS and BCL-1 cells, respectively.
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Cell Line:RAMOS Burkitt’s leukemia/lymphoma cells
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Concentration:100 nM
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Incubation Time:1 min; 5 min; 10 min
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Result:Inhibited H2O2-induced Y-phosphorylation of STAT3 in RAMOS cells.
体内実験
(DHQD) 2PHAL (10 mg/kg; intravenous bolus; two consecutive days; administration starting 1 day after inoculation) prevents overt leukemia and prolonged survival in SCID mice bearing RS4;11 or LC1;19 human BPL xenografts[1].
(DHQD) 2PHAL (10 mg/kg; intravenous bolus; two consecutive days; dosing initiated 1 day after leukemia cell inoculation) produces durable event-free survival in SCID mouse xenograft models of multiple chemotherapy-resistant human BPL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB.17 SCID (female, 6-8 weeks of age)[1]
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Dosage:10 mg/kg per dose
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Administration:i.v. bolus injection (0.2 mL/mouse); two consecutive days; starting 1 day after NALM-6 inoculation
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Result:In mice inoculated with 1×106 NALM-6 cells, C-61 produced a median EFS >120 d; cumulative proportion surviving event-free was 100% at 30 d, 100% at 60 d, 80% at 90 d, and 80% at 120 d.
Only 2 of 10 mice given C-61 developed leukemia with delayed-onset paraplegia at 75 and 80 d, whereas the remaining 8 became long-term survivors with no overt leukemia (paraplegia or hepatosplenomegaly) at elective killing at 121 d; median survival >121 d.
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Animal Model:CB.17 SCID (female, 6-8 weeks of age)[1]
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Dosage:10 mg/kg per dose
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Administration:i.v. bolus injection (0.2 mL/mouse); two consecutive days; starting 1 day after inoculation
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Result:In the combined RS4;11 and LC1;19 groups given C-61, all 20 mice remained healthy and had no signs of overt leukemia (paraplegia or hepatosplenomegaly) when electively killed at 121 d; median survival >121 d.
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Animal Model:CB.17 SCID (female, 6-8 weeks of age)[1]
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Dosage:10 mg/kg per dose
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Administration:i.v. bolus injection (0.2 mL/mouse); two consecutive days; starting 1 day after leukemia cell inoculation
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Result:In the composite C-61 group, median survival was >121 d and the 4-month EFS rate was 93%; cumulative proportion surviving event-free was 100% at 30 d, 100% at 60 d, 93% at 90 d, and 93% at 120 d.
Destroyed >99.9% of leukemia-initiating BPL cells in vivo across the three xenograft models.
- Kinase activity and phosphorylation assays
- Western Blot
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
化学情報
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CAS 番号 140853-10-7
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性状 Solid
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分子量 778.98
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分子式 C48H54N6O4
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Color White to off-white
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SMILES
CC[C@H]1C[N@]2[C@@](C[C@]1([H])CC2)([H])[C@H](C3=CC=NC(C=C4)=C3C=C4OC)OC(C5=C6C=CC=C5)=NN=C6O[C@@H](C7=CC=NC(C=C8)=C7C=C8OC)[C@](C[C@]9([H])CC%10)([H])N%10C[C@@H]9CC
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別名
C-61; SYKINH-61
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
体外:
DMSO : 5 mg/mL (6.42 mM; ultrasonic and warming and heat to 60°C; 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, stored under nitrogen). 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, stored under nitrogen). 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)
純度とドキュメンテーション
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データシート (304 KB)
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SDS (396 KB)
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- Deutsch - DE (396 KB)
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- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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 (protect from light, stored under nitrogen). 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 | 1.2837 mL | 6.4187 mL | 12.8373 mL | 32.0933 mL |
| 5 mM | 0.2567 mL | 1.2837 mL | 2.5675 mL | 6.4187 mL |
(DHQD)2PHAL 関連分類
HY-W008033 関連分類
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