PRT062607 Hydrochloride (Synonyms: PRT 062607 hydrochloride;PRT-062607 hydrochloride) |
| Catalog No.GC10499 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1370261-97-4
Sample solution is provided at 25 µL, 10mM.
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PRT062607 Hydrochloride is a highly selective and novel SYK inhibitor with IC50 value of 1 nM. Spleen tyrosine kinase (SYK) is a cytoplasmic tyrosine kinase and primarily expressed in hematopoietic cells including B-cells.
PRT062607 Hydrochloride is an orally bioavailable SYK inhibitor and its affinity for SYK is at least 80-fold greater than other kinases. In NHL cell lines, PRT062607 Hydrochloride inhibits SYK activation and induces caspase dependent apoptosis. Also, PRT062607 Hydrochloride inhibited SYK and caused apoptosis of the tumor B-cell line [1].
PRT062607 Hydrochloride effectively antagonize CLL cell survival after BCR triggering. Moreover, they inhibit the secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell transfer toward beneath stromal cells, the tissue homing chemokines CXCL13 and CXCL12 [2].
In a mouse xenograft model, mice dosed with all three concentrations (twice daily with 10, 15, or 20 mg/kg) of PRT062607 Hydrochloride were protected from Ramos tumor growth [1].
References:
[1]. Spurgeon SE, Coffey G, Fletcher LB, et al. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J Pharmacol Exp Ther, 2013, 344(2): 378-387.
[2]. Hoellenriegel J, Coffey GP, Sinha U, et al. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia, 2012, 26(7): 1576-1583.
| Cell experiment: [1] | |
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Cell lines |
Primary B-cells, SU-DHL6 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
1 μM, 24 hours |
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Applications |
To compare the relative sensitivity of primary versus tumor B-cells, the mixing experiments in which SU-DHL6 was combined with human whole blood and treated with P505-15 were performed. Under these conditions, whereas the tumor B-cell line underwent apoptosis in response to SYK inhibition, primary B-cells did not. |
| Animal experiment: [1] | |
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Animal models |
NOD/SCID mice injected with Ramos cells |
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Dosage form |
Oral administration, 10, 15, or 20 mg/kg, twice daily |
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Applications |
A statistically significant reduction in average tumor weight was achieved in all dosing groups relative to vehicle control. It revealed that submicromolar concentrations of P505-15 prevented tumor formation by an aggressive NHL cell line in mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Spurgeon S E, Coffey G, Fletcher L B, et al. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. Journal of Pharmacology and Experimental Therapeutics, 2013, 344(2): 378-387. | |
| Cas No. | 1370261-97-4 | SDF | |
| Synonyms | PRT 062607 hydrochloride;PRT-062607 hydrochloride | ||
| Chemical Name | 4-((3-(2H-1,2,3-triazol-2-yl)phenyl)amino)-2-(((1R,2R)-2-aminocyclohexyl)amino)pyrimidine-5-carboxamide hydrochloride | ||
| Canonical SMILES | NC(C1=C(NC2=CC(N3N=CC=N3)=CC=C2)N=C(N[C@H]4[C@H](N)CCCC4)N=C1)=O.Cl | ||
| Formula | C19H24ClN9O | M.Wt | 429.91 |
| Solubility | ≥ 21.5 mg/mL in DMSO, ≥ 83.2 mg/mL in Water with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3261 mL | 11.6303 mL | 23.2607 mL |
| 5 mM | 0.4652 mL | 2.3261 mL | 4.6521 mL |
| 10 mM | 0.2326 mL | 1.163 mL | 2.3261 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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