PP1

Alias: AGL 1872; EI 275;PP 1;AGL-1872; EI-275;PP-1;AGL1872; EI275;PP1
Cat No.:V0668 Purity: ≥98%
PP1 (known also as EI275; EI-275; PP-1; PP 1; AG1872; AG-1872) is a novel, potent and selective Src kinase inhibitor with potential antitumor activity.
PP1 Chemical Structure CAS No.: 172889-26-8
Product category: Src
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

PP1 (known also as EI275; EI-275; PP-1; PP 1; AG1872; AG-1872) is a novel, potent and selective Src kinase inhibitor with potential antitumor activity. It inhibits Lck/Fyn kinases with IC50 of 5 nM/6 nM. It exhibits excellent anti-proliferative activity in vitro and high in vivo antitumor efficacy.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In vitro, PP1 exhibits much lower doses of inhibition against Lck (IC50=5 nM) and FynT (IC50=6 nM) than against ZAP-70 (IC50>100 μM), JAK2 (IC50>50 μM), EGFR, and protein A. In human T cells, PP1 inhibits the production of the IL-2R gene and GM-CSF-induced IL-2 gene [1].
ln Vivo
Under in vivo conditions PP1 was suggested to suppress tyrosine phosphorylation and proliferation in T cells stimulated with anti-CD3 and mitogen. Studies using mice tumor model also showed that PP1 upregulated the expression of the IL-2 gene rather than the granulocyte macrophage colony-stimulating factor or the IL-2 receptor genes. Based on these, PP1 could be adopted as a useful agent to investigate the role of Lck and Fyn T cell activation.
Animal Protocol


References
[1]. Hanke JH, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J Biol Chem. 1996 Jan 12;271(2):695-701
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H19N5
Molecular Weight
281.36
CAS #
172889-26-8
SMILES
NC1=C2C(N(C(C)(C)C)N=C2C3=CC=C(C)C=C3)=NC=N1
Synonyms
AGL 1872; EI 275;PP 1;AGL-1872; EI-275;PP-1;AGL1872; EI275;PP1
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 4 mg/mL (14.2 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.5542 mL 17.7708 mL 35.5417 mL
5 mM 0.7108 mL 3.5542 mL 7.1083 mL
10 mM 0.3554 mL 1.7771 mL 3.5542 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
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