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My CartCAS：1247000-76-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
Qty：
Size：
| CAS | 1247000-76-5 |
| Name | (1E)-CFI-400437 dihydrochloride |
| Molecular Formula | C29H30Cl2N6O2 |
| Molecular Weight | 565.5 |
| Solubility | Soluble in DMSO ≥1mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD30347423 |
| SMILES | CN1CCN(CC1)C2=NC=C(C=C2)/C=C/C3=C4C=CC(=CC5=C(NC6=C5C=C(C=C6)OC)O)C=C4N=N3.Cl.Cl |
| InChIKey | NYCYUHRNBLSJAP-XPDSEMQYSA-N |
| InChI | InChI=1S/C29H28N6O2.2ClH/c1-34-11-13-35(14-12-34)28-10-5-19(18-30-28)4-8-26-22-7-3-20(16-27(22)33-32-26)15-24-23-17-21(37-2)6-9-25(23)31-29(24)36;;/h3-10，15-18，31，36H，11-14H2，1-2H3;2*1H/b8-4+，20-15 ;; |
| PubChem CID | 136351064 |
| Target Point | PLK4 |
| Passage | Cell Cycle |
| Background | (1E) - CFI-400437 dihydrochloride is an effective PLK4 and selective for other members of the PLK family. (1E) - CFI-400437 dihydrochloride also inhibits Aurora A， Aurora B， KDR， and FLT-3. It has anti proliferative activity. |
| Biological Activity | (1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A， Aurora B， KDR and FLT-3 with IC50s of 0.37， 0.21， 0.48， and 0.18 μM， respectively. Antiproliferative activity[1]. |
| IC50 | PLK3：0.6nM [1] |
| In Vivo | The plasma levels of(1E)-CFI-400437(50 mg/kg; IP; mice)dihydrochloride shows a Cmax of 92 ng/mL and AUC of 190 ng h/mL，respectively. The mouse plasma protein binding measurement for(1E)-CFI-400437 is 99%，i.e.，unbound compound in plasma is 1%[1]. |
| Data Literature Source | [1]. Laufer R，et al. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013;56(15):6069-6087 |
| Unit | Bottle |
| Specification | 1mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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