Luvixasertib hydrochloride (Synonyms: CFI-402257 hydrochloride)

Name: Luvixasertib hydrochloride
Brand: MedChemExpress
SKU: HY-101340A
Rating: 5.0 (8 reviews)

Cat. No.: HY-101340A Purity: 98.91%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Luvixasertib hydrochloride Chemical Structure

CAS No. : 1610677-37-6

Size	Price	Stock	Quantity
1 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 330	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2100	In-stock	Estimated Time of Arrival: December 31
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Based on 8 publication(s) in Google Scholar

Other Forms of Luvixasertib hydrochloride:

Luvixasertib In-stock

7 Publications Citing Use of MCE Luvixasertib hydrochloride

•bioRxiv. 2020 Apr.

: 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.

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Description

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^[1].

IC₅₀ & Target

IC50: 1.7 nM (TTK in vitro)^[1].

In Vitro

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 Cycle Analysis^[2]

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.

Western Blot Analysis^[2]

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.

In Vivo

CFI-402257 given orally QD shows dose-dependent activity in mice with established tumors from xenografted MDA-MB-231 human TNBC cells and MDA-MB-468 human TNBC cells in mice. CFI-402257 demonstrates antitumor activity in a platinum-resistant PDX model of high-grade serous ovarian cancer^[2].

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%.

Molecular Weight

535.04

Formula

C₂₈H₃₁ClN₆O₃

CAS No.

1610677-37-6

Appearance

Solid

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

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)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8690 mL	9.3451 mL	18.6902 mL
5 mM	0.3738 mL	1.8690 mL	3.7380 mL
10 mM	0.1869 mL	0.9345 mL	1.8690 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.13%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (253 KB) LCMS (93 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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Luvixasertib1610677-37-6CFI-402257CFI402257CFI 402257Mps1Monopolar spindle 1cancertumorInhibitorinhibitorinhibit

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Luvixasertib hydrochloride (Synonyms: CFI-402257 hydrochloride)

Customer Review

Other Forms of Luvixasertib hydrochloride:

Luvixasertib hydrochloride Related Antibodies

7 Publications Citing Use of MCE Luvixasertib hydrochloride

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Biological Activity

Purity & Documentation

References

Customer Review

Luvixasertib hydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Luvixasertib hydrochloride Related Classifications

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