PRT062607 HydrochlorideSYK inhibitor,potent and selective CAS# 1370261-97-4 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1370261-97-4 | SDF | Download SDF |
| PubChem ID | 56948527 | Appearance | Powder |
| Formula | C19H24ClN9O | M.Wt | 429.91 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | P505-15 Hydrochloride | ||
| Solubility | H2O : ≥ 50 mg/mL (116.30 mM) DMSO : ≥ 33 mg/mL (76.76 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[3-(triazol-2-yl)anilino]pyrimidine-5-carboxamide;hydrochloride | ||
| SMILES | C1CCC(C(C1)N)NC2=NC=C(C(=N2)NC3=CC=CC(=C3)N4N=CC=N4)C(=O)N.Cl | ||
| Standard InChIKey | RMNLLPXCNDZJMJ-IDVLALEDSA-N | ||
| Standard InChI | InChI=1S/C19H23N9O.ClH/c20-15-6-1-2-7-16(15)26-19-22-11-14(17(21)29)18(27-19)25-12-4-3-5-13(10-12)28-23-8-9-24-28;/h3-5,8-11,15-16H,1-2,6-7,20H2,(H2,21,29)(H2,22,25,26,27);1H/t15-,16+;/m0./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | PRT062607 (P505-15) HCl is a novel, highly selective inhibitor of Syk with IC50 of 1 nM, >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70. | |||||
| Targets | Syk | Fgr | MLK1 | |||
| IC50 | 1 nM | 81 nM | 88 nM | |||
| Cell experiment: [1] | |
| Cell lines | Primary B-cells, SU-DHL6 cells |
| 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. |
| Reacting condition | 1 μM, 24 hours |
| 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] | |
| Animal models | NOD/SCID mice injected with Ramos cells |
| Dosage form | Oral administration, 10, 15, or 20 mg/kg, twice daily |
| Application | 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. |
| 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. |
| 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. | |
PRT062607 Hydrochloride Dilution Calculator
PRT062607 Hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3261 mL | 11.6303 mL | 23.2607 mL | 46.5214 mL | 58.1517 mL |
| 5 mM | 0.4652 mL | 2.3261 mL | 4.6521 mL | 9.3043 mL | 11.6303 mL |
| 10 mM | 0.2326 mL | 1.163 mL | 2.3261 mL | 4.6521 mL | 5.8152 mL |
| 50 mM | 0.0465 mL | 0.2326 mL | 0.4652 mL | 0.9304 mL | 1.163 mL |
| 100 mM | 0.0233 mL | 0.1163 mL | 0.2326 mL | 0.4652 mL | 0.5815 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
Abstract
PRT062607, a highly selective SYK inhibitor with therapeutic activity for B-cell malignancies, inhibited SYK-mediated BCR signaling, prevented BCR-mediated splenomegaly, suppressed NHL tumor growth and decreased cell viability in NHL and CLL. The combination of PRT062607 and fludarabine exhibited synergistic effects against primary CLL cells.
Calcutta University
University of Minnesota
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University of Illinois at Chicago
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Harvard University
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The Institute of Cancer Research
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Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
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.
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