| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
CFI400945 is a potent, selective, and orally bioavailable PLK4 (polo-like kinase 4) inhibitor with IC50 value of 2.8 ±1.4 nM and potential antineoplastic activity. CFI-400945 selectively inhibits PLK4, causing apoptosis to be induced and mitosis to be disrupted. Inhibition of PLK4 also stops PLK4-overexpressing tumor cells from proliferating and dividing. Breast cell line and other tumor cell line growth can be markedly inhibited by CFI-400945. PLK4 is specifically inhibited in cells by CFI-400945, but it also exhibits some activity against AURKB, TRKA, TRKB, and Tie2/TEK (of 290 kinases, only 10 demonstrated more than 50% inhibition).
| Targets |
PLK4 (IC50 = 0.45 nM)
|
|
|---|---|---|
| ln Vitro |
UF010 primarily inhibits the G1/S transition with an increased G1 cell population and a decreased cell population in the S phase in a dose-dependent manner in cell-cycle analysis using MDA-MB-231 cells. In cell culture medium containing 10% fetal bovine serum, UF010 has a half-life of 15.8 hours[1].
|
|
| ln Vivo |
|
|
| Enzyme Assay |
Using an indirect ELISA detection system, active PLK4 is purified and used to measure PLK4 activity. FRET-based homogeneous assay kits from Invitrogen are used to measure the compound inhibition of PLK1, PLK2, PLK3, AURKA, and AUKB/INCENP. ATP concentrations of 25, 60, and 80 μM are used for PLK1, PLK2, and PLK3, and 20 and 128 μM are used for AURKA and AURKB/INCENP, respectively, in the assays.
|
|
| Cell Assay |
For six hours, HCT116 and A549 cells are exposed to either DMSO or etoposide (10 μM). One hour prior to cell lysis, TSA (0.2 μM), MS-275, and UF010 (2 μM) are added. Western blotting is performed on the whole cell lysates using antibodies to the specified proteins. It is found that PCNA is a loading control.
|
|
| Animal Protocol |
Adult female athymic CD1 nude mice
10 mg/kg via oral gavage |
|
| References |
| Molecular Formula |
C33H34N4O3
|
|
|---|---|---|
| Molecular Weight |
534.65
|
|
| Exact Mass |
534.26309096
|
|
| CAS # |
1338806-73-7
|
|
| Related CAS # |
|
|
| SMILES |
C[C@@H]1CN(C[C@@H](O1)C)CC2=CC=C(C=C2)/C=C/C3=NNC4=C3C=CC(=C4)[C@@H]5C[C@]56C7=C(C=CC(=C7)OC)NC6=O
|
|
| InChi Key |
DADASRPKWOGKCU-FVTQAUBDSA-N
|
|
| InChi Code |
InChI=1S/C33H34N4O3/c1-20-17-37(18-21(2)40-20)19-23-6-4-22(5-7-23)8-12-29-26-11-9-24(14-31(26)36-35-29)28-16-33(28)27-15-25(39-3)10-13-30(27)34-32(33)38/h4-15,20-21,28H,16-19H2,1-3H3,(H,34,38)(H,35,36)/b12-8+/t20-,21+,28-,33-/m0/s1
|
|
| Chemical Name |
(2'S,3R)-2'-[3-[(E)-2-[4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]-5-methoxyspiro[1H-indole-3,1'-cyclopropane]-2-one
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8704 mL | 9.3519 mL | 18.7038 mL | |
| 5 mM | 0.3741 mL | 1.8704 mL | 3.7408 mL | |
| 10 mM | 0.1870 mL | 0.9352 mL | 1.8704 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03187288 | Active Recruiting |
Drug: CFI-400945 Fumarate | Relapsed Cancer Refractory Cancer |
University Health Network, Toronto |
May 25, 2018 | Phase 1 |
| NCT04176848 | Active Recruiting |
Drug: CFI-400945 Drug: Durvalumab |
Breast Cancer | Canadian Cancer Trials Group | December 19, 2019 | Phase 2 |
| NCT03624543 | Active Recruiting |
Drug: CFI-400945 | Breast Cancer | Canadian Cancer Trials Group | February 14, 2019 | Phase 2 |
| NCT03385655 | Active Recruiting |
Drug: Adavosertib Drug: CFI-400945 |
Prostate Cancer | Canadian Cancer Trials Group | August 1, 2018 | Phase 2 |
| NCT04730258 | Recruiting | Drug: CFI-400945 Drug: Azacitidine |
AML MDS |
Treadwell Therapeutics, Inc | April 16, 2021 | Phase 1 Phase 2 |
CFI-400945 Is a PLK4-Selective Inhibitor.Cancer Cell.2014 Aug 11;26(2):163-76. |
|---|
CFI-400945 Causes Centriole Duplication Defects in Cancer Cells.Cancer Cell.2014 Aug 11;26(2):163-76. |
CFI-400945 Increases the PLK4 Protein Level at Centrioles.Cancer Cell.2014 Aug 11;26(2):163-76. |
Response Profile of CFI-400945 versus Breast Cancer Cell Lines.Cancer Cell.2014 Aug 11;26(2):163-76. |
|---|
In Vivo Characterization of the Anticancer Potential CFI-400945 on Human Xenograft Tumors.Cancer Cell.2014 Aug 11;26(2):163-76. |
In Vivo Effect of CFI-400945 on Human Xenograft Tumors.Cancer Cell.2014 Aug 11;26(2):163-76. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
