Src kinase inhibitor PP2
PP2
CAS: 172889-27-9
Molecular Formula: C15H16ClN5
Src kinase inhibitor PP2 - Names and Identifiers
Src kinase inhibitor PP2 - Physico-chemical Properties
| Molecular Formula | C15H16ClN5 |
| Molar Mass | 301.77 |
| Density | 1.35±0.1 g/cm3(Predicted) |
| Boling Point | 493.5±40.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 3 mg/ml with warming). |
| Appearance | Off-white solid |
| Color | Off-white |
| pKa | 3.96±0.30(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
| In vitro study | PP2(5 μm) acts on NIH3T3 and NIH-RET/PTC3 cell lysates to inhibit phosphorylation and signaling of RET/PTC1 tumor protein in vivo. PP2(5 μm) acts on NIH3T3 fibroblasts transforming RET/PTC1, and two human papillary thyroid carcinoma cell lines TPC1 and FB2 carrying spontaneous RET/PTC1 rearrangements, inhibits serum-independent growth. PP2 (5 μm) inhibited TPC1 cell type I collagen matrix invasion. PP2 inhibits Src by binding to a region of the molecule that does not overlap with the ATP binding domain. PP2(20 μm) inhibited HT29 cell growth by 40-50%. After 1 hour of treatment, this concentration reduced Src activity and maintained a 35% inhibition of Src activity for 2 days. PP2(100 mM) decreased Src activity in HT29 cells in a dose-dependent manner. PP2(1 mM-100 mM) inhibits human colon cancer cells (HT29, SW480, and PMCO1), hepatoma cells (PLC/PRF/5, KYN-2, Li7, and HepG2), and growth of breast cancer cells (MCF-7, MDA-MB-468, and BT-474) in a dose-dependent manner. PP2(20 μm) significantly promoted the polymerization of most cancer cells (HT29, SW480, PMCO1, PLC/PRF/5, KYN-2, Li7, MCF-7, and MDA-MB-468), this effect is E-cadherin dependent. PP2(20 μm) acts on cancer cells, enhances E-cadherin expression, and strongly promotes the Association of E-cadherin with the actin cytoskeleton. PP2(20 μm) acts on HT29 cells to enhance α-catenin, β-catenin, And γ-catenin expression, while acting on PLC/PRF/5 and MCF-7 cells, the total protein level of α-catenin did not change, but the levels of β-catenin and γ-catenin increased slightly. PP2 inhibited the proliferation of two cervical cancer cells (HeLa and SiHa) in a time-and dose-dependent manner. PP2(10 μm) acts on HeLa and SiHa cells to down-regulate pSrc-Y416, pEGFR-Y845, and-Y1173 expression levels. PP2(10 μm) upregulated p21(Cip1) and p27(Kip1) in HeLa and SiHa cells, and downregulated cyclin A and cyclin-dependent kinase -2 in HeLa cells,-4 (Cdk-2,-4) expression, and down-regulation of cyclin B and Cdk-2 expression in SiHa cells, can regulate cell cycle arrest. |
| In vivo study | Treatment of SCID mice inoculated with HT29 cells in the spleen with PP2 at a dose of 5 mg/kg per day reduced the growth rate of primary tumors compared to controls. Treatment of SCID mice inoculated with HT29 cells in the spleen with PP2 at a dose of 5 mg/kg per day significantly reduced the relative liver weight and the amount of liver metastasis compared with the control group. Intraperitoneal injection of PP2 at a dose of 1.5 mg/kg in rats with focal cerebral ischemia injury reduced the infarct size by about 50%. Compared with the control group, rats with focal cerebral ischemia injury were treated intraperitoneally with PP2 at a dose of 1.5 mg/kg, which had better neurological function scores. |
Src kinase inhibitor PP2 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
Src kinase inhibitor PP2 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.314 ml | 16.569 ml | 33.138 ml |
| 5 mM | 0.663 ml | 3.314 ml | 6.628 ml |
| 10 mM | 0.331 ml | 1.657 ml | 3.314 ml |
| 5 mM | 0.066 ml | 0.331 ml | 0.663 ml |
Last Update：2024-01-02 23:10:35
Src kinase inhibitor PP2 - Reference Information
| biological activity | PP2 is a Src family kinase inhibitor, which effectively inhibits Lck/Fyn,IC50 is 4 nM/5 nM, which is about 100 times less effective on EGFR and inhibits ZAP-70, JAK2 and PKA activities. PP2 (AG 1879, AGL 1879) is a Src family kinase inhibitor that effectively inhibits Lck/Fyn with an IC50 of 4 nM/5 nM in a cell-free assay, the effect on EGFR was about 100 times lower, and there was no activity on ZAP-70,JAK2 and PKA. |
| Target | Value |
| LCK (Cell-free assay) | 4 nM |
| Fyn (Cell-free assay) | 5 nM |
Last Update：2024-04-09 20:52:54
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Product Name: AGL 1879 Visit Supplier Webpage Request for quotationCAS: 172889-27-9
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: PP2 Visit Supplier Webpage Request for quotationCAS: 172889-27-9
Tel: +16314854226
Email: info@bocsci.com
Mobile: +16314854226
Linkedin: https://www.linkedin.com/company/boc-sciences
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Product Name: PP2 Visit Supplier Webpage Request for quotationCAS: 172889-27-9
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
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Product Name: PP-2 Visit Supplier Webpage Request for quotationCAS: 172889-27-9
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
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Tel: 18301782025
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View History
Src kinase inhibitor PP2
环丁基丙氨酸
Benzenesulfonamide, N-[(2-bromophenyl)phenylmethyl]-2,4,6-tris(1-methylethyl)-
叔丁基哌啶-3-基氨基甲酸酯
白杨素 6-C-Β-D-葡萄糖-8-C-Α-L-阿拉伯糖苷
RAC色氨酸EP杂质G HCL
5-乙炔-2-氟苯甲醛
N6-苯甲酰-2'-甲氧基腺苷
diglycol monomethyl ether
三月桂醇柠檬酸酯
环丁基丙氨酸
Benzenesulfonamide, N-[(2-bromophenyl)phenylmethyl]-2,4,6-tris(1-methylethyl)-
叔丁基哌啶-3-基氨基甲酸酯
白杨素 6-C-Β-D-葡萄糖-8-C-Α-L-阿拉伯糖苷
RAC色氨酸EP杂质G HCL
5-乙炔-2-氟苯甲醛
N6-苯甲酰-2'-甲氧基腺苷
diglycol monomethyl ether
三月桂醇柠檬酸酯