Luvixasertib hydrochloride
Based on 7 publication(s) in Google Scholar
CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 1610677-37-6
- Formula: C28H31ClN6O3
- Molecular Weight:535.04
-
Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Kinase Inhibitor Library
HY-L009
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Cytoskeleton Compound Library
HY-L060
-
Orally Active Compound Library
HY-L061
-
Chemical Probe Library
HY-L063
-
Targeted Diversity Library
HY-L099
-
Highly Selective Inhibitors Library
HY-L158
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Anti-Aging Compound Library Mini
HY-L034M
-
MCE Bioactive Compound Library
HY-L001V
-
Kinase Inhibitor Library Mini
HY-L009M
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) Luvixasertib hydrochloride
More
Customer Validation & Images
-
WB
Biological Activity
IC50: 1.7 nM (TTK in vitro)[1].
CFI-402257 is highly selective to TTK. CFI-402257 is tested against a panel of human kinases at 1 μM and inhibits none of the 262 kinases tested. CFI-402257 is a potent inhibitor of cell growth[1].
CFI-402257 (200 nM, 6 h) causes a massive increase in chromosome missegregations[2].
CFI-402257 (0, 50 or 100 nM) induces a dose-dependent dysregulation of the cell cycle, resulting in an increase in the frequency of cells exhibiting an aneuploid DNA content[2].
CFI-402257 exhibits effects consistent with Mps1 kinase inhibition, specifically SAC inactivation, leading to chromosome missegregation, aneuploidy, and ultimately cell death[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HCT116 cells.
-
Concentration:0 nM, 50 nM, 100 nM, 300 nM, 1000 nM, 3000 nM.
-
Incubation Time:48 hours
-
Result:Resulted in an increase in the frequency of cells exhibiting an aneuploid DNA content.
-
Cell Line:HCT116 cells.
-
Concentration:0 nM, 50 nM or 100 nM.
-
Incubation Time:8, 16, 24 and 48 hours.
-
Result:CFI-402257-induced aneuploidy was accompanied by a progressive accumulation of apoptotic cells that were detectable as early as 16 h following treatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Xenografted MDA-MB-231 human TNBC cells and MDA-MB-468 human TNBC cells in mice[2].
-
Dosage:5, 6 mg/kg.
-
Administration:Oral gavage, daily.
-
Result:Xenografted MDA-MB-231 human TNBC cells: 5 mg/kg, tumor growth inhibition (TGI) = 74%; 6 mg/kg, TGI = 89%.
Xenografted MDA-MB-468 human TNBC cells: 5 mg/kg, tumor growth inhibition (TGI) = 75%; 6 mg/kg, TGI = 94%.
-
Animal Model:PDX model of high-grade serous ovarian cancer[2].
-
Dosage:6.5, 7.5 mg/kg.
-
Administration:Oral gavage, daily.
-
Result:6.5 mg/kg, tumor growth inhibition (TGI) = 61%; 7.5 mg/kg, TGI = 97%.
Chemical Information
-
CAS No. 1610677-37-6
-
Appearance Solid
-
Molecular Weight 535.04
-
Formula C28H31ClN6O3
-
Color Light yellow to yellow
-
SMILES
CC1=CC(C2=C3N=C(OC4=CN=CC=C4)C=C(NC[C@@H]5C[C@@](O)(C)C5)N3N=C2)=CC=C1C(NC6CC6)=O.Cl
-
Synonyms
CFI-402257 hydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (7)
-
Journal Impact Factor
-
Most Recent
-
Cancer Discov
Cells Lacking the RB1 Tumor Suppressor Gene Are Hyperdependent on Aurora B Kinase for Survival. [Abstract]2019 Feb;9(2):230-247. PMID: 30373918
Luvixasertib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2019 Feb;9(2):230-247. [Abstract]
Western analysis of protein expression in different concentrations of CFI-402257 treatment.
-
Commun Biol
Integrated genomics and comprehensive validation reveal drivers of genomic evolution in esophageal adenocarcinoma. [Abstract]2021 May 24;4(1):617. PMID: 34031527 -
Oncol Rep
Energy‑stress‑mediated activation of AMPK sensitizes MPS1 kinase inhibition in triple‑negative breast cancer. [Abstract]2024 Aug;52(2):101. PMID: 38904203 -
PLoS Genet
Barrier-to-autointegration factor protects against the cGAS-STING response to chromatin bridges. [Abstract]2026 Jun 3;22(6):e1012191. PMID: 42234713 -
Front Oncol
Dual TTK/PLK1 inhibition has potent anticancer activity in TNBC as monotherapy and in combination. [Abstract]2024 Aug 9:14:1447807. PMID: 39184047 -
-
Solvent & Solubility
DMSO : 100 mg/mL (186.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
References
[1]. Liu Y, et al. Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent. ACS Med Chem Lett. 2016 May 6;7(7):671-5. [Content Brief]
[2]. Mason JM, et al. Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127-3132. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8690 mL | 9.3451 mL | 18.6902 mL | 46.7255 mL |
| 5 mM | 0.3738 mL | 1.8690 mL | 3.7380 mL | 9.3451 mL | |
| 10 mM | 0.1869 mL | 0.9345 mL | 1.8690 mL | 4.6725 mL | |
| 15 mM | 0.1246 mL | 0.6230 mL | 1.2460 mL | 3.1150 mL | |
| 20 mM | 0.0935 mL | 0.4673 mL | 0.9345 mL | 2.3363 mL | |
| 25 mM | 0.0748 mL | 0.3738 mL | 0.7476 mL | 1.8690 mL | |
| 30 mM | 0.0623 mL | 0.3115 mL | 0.6230 mL | 1.5575 mL | |
| 40 mM | 0.0467 mL | 0.2336 mL | 0.4673 mL | 1.1681 mL | |
| 50 mM | 0.0374 mL | 0.1869 mL | 0.3738 mL | 0.9345 mL | |
| 60 mM | 0.0312 mL | 0.1558 mL | 0.3115 mL | 0.7788 mL | |
| 80 mM | 0.0234 mL | 0.1168 mL | 0.2336 mL | 0.5841 mL | |
| 100 mM | 0.0187 mL | 0.0935 mL | 0.1869 mL | 0.4673 mL |
Luvixasertib hydrochloride Related Classifications
HY-101340A Related Classifications
Powered by Bioz