2. Protein Tyrosine Kinase/RTK Cytoskeleton Cell Cycle/DNA Damage MAPK/ERK Pathway Apoptosis
  3. Pyk2 PAK Mixed Lineage Kinase FAK Src Apoptosis Syk
  4. PRT062607 Hydrochloride

PRT062607 Hydrochloride  (Synonyms: P505-15 Hydrochloride)

Cat. No.: HY-15323 Purity: 98.68%
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PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models.

For research use only. We do not sell to patients.

PRT062607 Hydrochloride Chemical Structure

PRT062607 Hydrochloride Chemical Structure

CAS No. : 1370261-97-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 172 In-stock
Solid
5 mg USD 156 In-stock
10 mg USD 238 In-stock
25 mg USD 420 In-stock
50 mg USD 634 In-stock
100 mg USD 980 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of PRT062607 Hydrochloride:

PRT062607 Hydrochloride Related Antibodies

Top Publications Citing Use of Products

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

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Lck Fyn Blk

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models[1][2].

IC50 & Target

Lck

249 nM (IC50, [2])

PAK5

166 nM (IC50, [2])

In Vitro

PRT062607 Hydrochloride also has significant activity against a variety of kinases, with IC50s of 81 nM (Fgr), 88 nM (MLK1), 123 nM (Yes), 139 nM (Flt3), 166 nM (PAK5), 192 nM (Lyn), 244 nM (cSRC), 249 nM (Lck), 108 nM (Pyk), 415 nM (FAK), 1.05 nM (ZAP-70)[1].
PRT062607 Hydrochloride (0.01-2 μM; 3 d) Inhibits Phosphorylation of ERK(Y204), AKT(S473) and SYK(Y352) in Ramos cells, and inhibition of BLNK Tyr84 phosphorylation[1][2].
PRT062607 Hydrochloride (2 μM; 24 h) in SU-DHL6 cells Induces apoptosis in human whole blood[1].
In human whole blood, P505-15 can effectively inhibit B cell antigen receptor-mediated B cell signaling and activation (IC50: 0.27 and 0.28 μM) and Fc receptor 1-mediated induced basophil degranulation (IC50: 0.15 μM)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PRT062607 Hydrochloride Related Antibodies

Western Blot Analysis

Cell Line: Ramos cells[1], SUDHL4 cells[2]
Concentration: 0.01, 0.025, 0.064, 0.16, 0.4, 2.5 μM
Incubation Time: 3 days
Result: Resulted not entirely concentration-dependent and complete inhibition on ERK (Y204) and AKT (S473) phosphorylation, Lyn phosphorylation of SYK at Y352.
Inhibited BLNK Tyr84 phosphorylation in a concentration dependent manner, while whitout inhibitory effect on Lyn activity.
Potently inhibited BCR-mediated pERK Tyr204 in the Ramos B cell line, without suppressing PMA-mediated pERK Tyr204.
In Vivo

PRT062607 Hydrochloride produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. PRT062607 Hydrochloride (15, 30 mg/kg; po; bid; 5 d) causes SYK inhibition in mice and prevents BCR-induced splenomegaly in mice[1].
PRT062607 Hydrochloride (15 mg/kg; po ; bid; 5 d) SYK inhibition in mice prevents Ramos tumor formation in mouse xenograft models[1].
PRT062607 Hydrochloride (10-20 mg/kg; po; bid, ) prevents BCR mediated splenomegaly and significantly inhibited NHL tumor growth in xenograft models[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: anti-IgD Stimulated Mouse Inflammation Model[1]
Dosage: 10 mg/kg, 15 mg/kg, 20 mg/kg
Administration: po; bid for 5 days
Result: Suppressed mouse B-cell activation following stimulation with this anti-IgD.
Animal Model: Ramos Tumor Xenograft Model in NOD/SCID mice[1]
Dosage: 15 mg/kg, 30 mg/kg
Administration: po; bid; terminated when tumor weights began reaching approximately 1.5 mg, at which time tumors were excised and weighed.
Result: Protected mouse from Ramos tumor growth in vivo.
Clinical Trial
Molecular Weight

429.91

Formula

C19H24ClN9O
CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

NC(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(N4N=CC=N4)=C3)=O.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (116.30 mM)

DMSO : ≥ 33 mg/mL (76.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (116.30 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.68%

COA (257 KB) LCMS (268 KB)

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 (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
DMSO / H2O 1 mM 2.3261 mL 11.6303 mL 23.2607 mL 58.1517 mL
5 mM 0.4652 mL 2.3261 mL 4.6521 mL 11.6303 mL
10 mM 0.2326 mL 1.1630 mL 2.3261 mL 5.8152 mL
15 mM 0.1551 mL 0.7754 mL 1.5507 mL 3.8768 mL
20 mM 0.1163 mL 0.5815 mL 1.1630 mL 2.9076 mL
25 mM 0.0930 mL 0.4652 mL 0.9304 mL 2.3261 mL
30 mM 0.0775 mL 0.3877 mL 0.7754 mL 1.9384 mL
40 mM 0.0582 mL 0.2908 mL 0.5815 mL 1.4538 mL
50 mM 0.0465 mL 0.2326 mL 0.4652 mL 1.1630 mL
60 mM 0.0388 mL 0.1938 mL 0.3877 mL 0.9692 mL
H2O 80 mM 0.0291 mL 0.1454 mL 0.2908 mL 0.7269 mL
100 mM 0.0233 mL 0.1163 mL 0.2326 mL 0.5815 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.

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PRT062607 Hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PRT0626071370261-97-4P505-15PRT 062607PRT-062607Pyk2PAKMixed Lineage KinaseFAKSrcApoptosisSykProline-rich tyrosine kinase 2p21 activated kinasesMLKsPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseSpleen tyrosine kinaseSyk inhibitorsInhibitorinhibitorinhibit

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