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Purity: ≥98%
PP2 (also known as AG 1879; AG-1879) a novel, potent, reversible, and ATP-competitive and selective Src family kinase inhibitor with potential anticancer activity. It inhibits Lck/Fyn kinases with IC50s of 4 nM/5 nM in cell-free assays, and is less potent to or inactive for EGFR, ZAP-70, JAK2 and PKA. PP2 is a chemical substance frequently used in cancer research. PP2 induces slowing in the growth rate of tumors in SCID mice inoculated HT29 cells in the spleen. It strongly inhibits the kinases Lck (IC50=4 nM), Fyn (5 nM) and Hck (5 nM), shows weaker inhibition of EGFR (480 nM) and practically no inhibition of ZAP-70 (100 µM) and JAK2 (50 µM).
| ln Vitro |
At 10 μM, the impact of PP2 on cell proliferation was not statistically significant, indicating that the PP2 effect on gemcitabine cytotoxicity at this low dosage is likely due to gemcitabine-induced cell proliferation rather than a direct antiproliferative action. elevated toxicity. Growth was progressively suppressed at 20 μM, which is in accordance with findings from other human cancer cell lines. While we employed 10 μM PP2, it has been documented that PP2 at higher concentrations inhibits other intracellular kinases [2]. The most popular Src family kinase inhibitor on the market is PP2. With an in vitro IC50 of roughly 5 nM, PP2 suppresses Src family kinase activity. Complete Src family kinase inhibition in cell culture is typically achieved at a dosage of 10 μM [3].
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| ln Vivo |
In the PP2 treatment group, the tumor growth inhibition rate is 25%, while in the Gemcitabine treatment group, it is 5% (P>0.05). When combined, PP2 and gemcitabine result in a 98% (P<0.05) tumor growth suppression rate. In 100% of the control and gemcitabine-treated groups, liver metastases occurred; in the PP2-treated group, 88% of the liver metastases formed. In the group receiving combined treatment with PP2 and Gemcitabine, there are no observable metastases (P<0.05)[2].
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| References |
[1]. Hanke JH, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck-and FynT-dependentT cell activation. J Biol Chem. 1996 Jan 12;271(2):695-701.
[2]. Duxbury MS, et al. Inhibition of SRC tyrosine kinase impairs inherent and acquired Gemcitabine resistance in human pancreatic adenocarcinoma cells. Clin Cancer Res. 2004 Apr 1;10(7):2307-18 [3]. Summy JM, et al. AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes. Mol Cancer Ther. 2005 D [4]. Inoue A, et al. Phosphorylation of NMDA receptor GluN2B subunit at Tyr1472 is important for trigeminal processing of itch. Eur J Neurosci. 2016 Oct;44(7):2474-2482 |
| Molecular Formula |
C15H16CLN5
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| Molecular Weight |
431.53
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| CAS # |
172889-27-9
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| Related CAS # |
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| SMILES |
NC1=C2C(N(C(C)(C)C)N=C2C3=CC=C(Cl)C=C3)=NC=N1
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| InChi Key |
PBBRWFOVCUAONR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)
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| Chemical Name |
1-(tert-butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
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| Synonyms |
AG 1879; AG-1879; PP2; PP-2; PP 2; AG1879.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (9.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 4% DMSO+30% PEG 300+ddH2O:5 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3173 mL | 11.5867 mL | 23.1734 mL | |
| 5 mM | 0.4635 mL | 2.3173 mL | 4.6347 mL | |
| 10 mM | 0.2317 mL | 1.1587 mL | 2.3173 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.
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06012734 | Not yet recruiting | Drug: LB-100 Drug: Atezolizumab |
Metastatic Microsatellite-stable Colorectal Cancer |
The Netherlands Cancer Institute | December 2023 | Phase 1 |
| NCT06065462 | Recruiting | Drug: Dostarlimab Drug: LB-100 |
Ovarian Clear Cell Carcinoma | M.D. Anderson Cancer Center | November 10, 2023 | Phase 1 Phase 2 |
| NCT00807365 | Terminated Has Results | Drug: GHRH | Elderly | Johns Hopkins University | December 17, 2007 | Phase 2 |
| NCT00005592 | Completed | Biological: 90-Y-ibritumomab tiuxetan Biological: rituximab |
Lymphoma | University of Alabama at Birmingham | November 1999 | Phase 2 |
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