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- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
Biological Activity
Crenolanib (CP-868596) is an orally bioavailable, selective small molecule inhibitor of the PDGFR tyrosine kinase, inhibiting both PDGFRA and PDGFRB at picomolar concentrations.
Targets
| PDGFRα (CHO cells) | PDGFRβ (CHO cells) | FLT3 | ||
| 2.1 nM(Kd) | 3.2 nM(Kd) | 0.74 nM (Kd) |
| In vitro (25°C) | DMSO | Warmed: 84 mg/mL (189.38 mM) | |
| Water | Insoluble | ||
| Ethanol | 7 mg/mL (15.78 mM) | ||
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 28 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 | 22.55 mL | 112.74 mL | 225.48 mL |
| 0.5 mM | 4.51 mL | 22.55 mL | 45.1 mL |
| 1 mM | 2.25 mL | 11.27 mL | 22.55 mL |
| 5 mM | 0.45 mL | 2.25 mL | 4.51 mL |
*The above data is based on the productmolecular weight 443.5 . 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 | A11052 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 670220-88-9 |
| Formula | C26H29N5O2 |
| M. Wt | 443.5 |
| Purity | >98% |
| Synonyms | CP868596, CP 868596 |
| SMILES | CC1(COC1)COC2=CC3=C(C=C2)N(C=N3)C4=NC5=C(C=CC=C5N6CCC(CC6)N)C=C4 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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