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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Yu B, .et al. Pharmacokinetics and metabolism of ulixertinib in rat by liquid chromatography combined with electrospray ionization tandem mass spectrometry, J Sep Sci, 2020, Jan 22 PMID: 31970927
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Saki Omote, .et al. Effect of tyrosine kinase inhibitors on renal handling of creatinine by MATE1, Sci Rep, 2018, 8: 9237 PMID: 29915248
- Arakawa H, .et al. Inhibitory Effect of Crizotinib on Creatinine Uptake by Renal Secretory Transporter OCT2, J Pharm Sci, 2017, Sep;106(9):2899-2903 PMID: 28336299
Biological Activity
PF-2341066 (Crizotinib) is an inhibitor of the c-Met kinase and the NPM-ALK. PF-2341066 inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM).
Targets
| c-Met (A549, MDA-MB-231, GTL-16, HT29, 786-O, Colo-205, A498 cells) | ALK (Karpas299 cells) | |||
| 11 nM | 24 nM |
| In vitro (25°C) | DMSO | 8 mg/mL (17.76 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 5% DMSO+30% PEG 300+dd H2O | 4 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 22.21 mL | 111.04 mL | 222.07 mL |
| 0.5 mM | 4.44 mL | 22.21 mL | 44.41 mL |
| 1 mM | 2.22 mL | 11.1 mL | 22.21 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.44 mL |
*The above data is based on the productmolecular weight 450.3. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10712 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 877399-52-5 |
| Formula | C21H22Cl2FN5O |
| M. Wt | 450.3 |
| Purity | >98% |
| Synonyms | PF02341066 |
| SMILES | C[[email protected]](C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
Datasheet
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