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

PRT062607 acetate  (Synonyms: P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate)

Cat. No.: HY-15324 Purity: 99.83%
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PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models..

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

PRT062607 acetate Chemical Structure

PRT062607 acetate Chemical Structure

CAS No. : 1370261-98-5

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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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Based on 3 publication(s) in Google Scholar

Other Forms of PRT062607 acetate:

PRT062607 acetate Related Antibodies

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

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Lck Fyn Blk

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Description

PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate 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 acetate also has significant activity against multiple 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 acetate (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 acetate (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 acetate 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 acetate produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. PRT062607 acetate (15, 30 mg/kg; po; bid; 5 d) causes SYK inhibition in mice and prevents BCR-induced splenomegaly in mice[1].
PRT062607 acetate (15 mg/kg; po ; bid; 5 d) SYK inhibition in mice prevents Ramos tumor formation in mouse xenograft models[1].
PRT062607 acetate (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.
Molecular Weight

453.50

Formula

C21H27N9O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

DMSO : 10 mg/mL (22.05 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2051 mL 11.0254 mL 22.0507 mL
5 mM 0.4410 mL 2.2051 mL 4.4101 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.

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

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Concentration
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

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Concentration (final)

C2

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Volume (final)

V2

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

Dosage

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 1 mM 2.2051 mL 11.0254 mL 22.0507 mL 55.1268 mL
5 mM 0.4410 mL 2.2051 mL 4.4101 mL 11.0254 mL
10 mM 0.2205 mL 1.1025 mL 2.2051 mL 5.5127 mL
15 mM 0.1470 mL 0.7350 mL 1.4700 mL 3.6751 mL
20 mM 0.1103 mL 0.5513 mL 1.1025 mL 2.7563 mL
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PRT062607 acetate 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:

PRT0626071370261-98-5P505-15PRT-2607BIIB-057PRT 062607PRT-062607PRT2607PRT 2607BIIB057BIIB 057Pyk2PAKMixed Lineage KinaseFAKSrcApoptosisSykProline-rich tyrosine kinase 2p21 activated kinasesMLKsPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseSpleen tyrosine kinaseSyk inhibitorsInhibitorinhibitorinhibit

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