(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.
For research use only. We do not sell to patients.
- Purity : 98.0%
- CAS No.: 140853-10-7
- Formula: C48H54N6O4
- Molecular Weight:778.98
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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(R)-(+)-2,2-Dimethyl-1,3-dioxolane-4-carboxaldehydeStarting Material
Biological Activity
Description
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Syk |
STAT3 |
In Vitro
(DHQD) 2PHAL (C-61) induces apoptosis in SYK+ primary leukemia cells[1].
(DHQD) 2PHAL (SYKINH-61) (1-100 nM; 30 min RAMOS; 1-10 min BCL-1) prevents oxidative stress-induced SYK tyrosine phosphorylation in RAMOS and BCL-1 B-lineage lymphocytes[2].
(DHQD) 2PHAL (100 nM; 1-10 min) inhibits H2O2-induced STAT3 Y705 phosphorylation in RAMOS Burkitt leukemia/lymphoma cells[2].
(DHQD) 2PHAL eliminates PV-induced STAT3 DNA-binding activity in human B-cell lines[2].
(DHQD) 2PHAL inhibits constitutively active native SYK in NALM-6 B-lineage ALL cells without altering SYK protein levels[2].
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.
In Vivo
(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
Chemical Information
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CAS No. 140853-10-7
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Appearance Solid
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Molecular Weight 778.98
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Formula 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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Synonyms
C-61; SYKINH-61
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (303 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
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 Related Classifications
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