PP121
PP121 is a dual inhibitor of tyrosine and phosphoinositide kinases [1].
PP121 is found to inhibit both tyrosine kinases and PI3-Ks but not serine-threonine kinases. It potently inhibits p110α, p110β, p110γ, p110δ, DNA-PK and mTOR with IC50 values of 52nM, 1.4μM, 1.1μM, 150nM, 60nM and 10nM, respectively. For the tyrosine kinases, PP121 shows inhibition with IC50 values of 21nM, 4nM, 10nM,55nM, 550nM, 220nM and <1nM for Ab1, Hck, Src, VEGFR2, EGFR, EphB4 and PDGFR, respectively [1].
In cells, PP121 can reverse v-Src mediated cellular transformation and restore actin stress fiber staining. PP121 also potently inhibits the mutant Ret kinase with IC50 value less than 1nM in thyroid tumors34. Furthermore, PP121 is found to evade drug resistance through redundantly targeting Bcr-Abl mediated cell survival and PI3-K/mTOR mediated cell proliferation [1].
References:
[1] Apsel B, Blair J A, Gonzalez B, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nature chemical biology, 2008, 4(11): 691-699.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 319.37 |
| Cas No. | 1092788-83-4 |
| Formula | C17H17N7 |
| Solubility | insoluble in H2O; ≥1.65 mg/mL in EtOH with gentle warming and ultrasonic; ≥15.95 mg/mL in DMSO |
| Chemical Name | 1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazolo[3,4-d]pyrimidin-4-amine |
| SDF | Download SDF |
| Canonical SMILES | C1CCC(C1)N2C3=C(C(=N2)C4=CN=C5C(=C4)C=CN5)C(=NC=N3)N |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 values of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM,respectively. | |||||
| Targets | PDGFR | Hck | VEGFR | mTOR | Src | Abl |
| IC50 | 2 nM | 8 nM | 12 nM | 13 nM | 14 nM | 18 nM |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
