Darovasertib (Synonyms: LXS196; IDE196)

Name: Darovasertib
Brand: MedChemExpress
SKU: HY-101569
Rating: 5.0 (4 reviews)

Cat. No.: HY-101569 Purity: 99.78%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC₅₀ values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 1874276-76-2

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
2 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE Darovasertib

Cell Proliferation/Viability Assay

: Darovasertib purchased from MedChemExpress. Usage Cited in: Patent. US20210230154A1.; Darovasertib (0-10 μM) inhibited 92-1 cells growth in a dose-dependent manner.

: Darovasertib purchased from MedChemExpress. Usage Cited in: Patent. US20210230154A1.; Darovasertib (0-10 μM) inhibited MP-14 cells growth in a dose-dependent manner.

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•Related Screening Libraries:

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View All PKC Isoform Specific Products:

View All Isoforms

PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[2]

PKCα

1.9 nM (IC₅₀)

PKCθ

0.4 nM (IC₅₀)

GSK3β

3.1 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
SK-MEL-28	IC₅₀	> 10 μM Compound: 20; LXS196	Cytotoxicity against human SK-MEL-28 cells expressing B-Raf V600E mutant Cytotoxicity against human SK-MEL-28 cells expressing B-Raf V600E mutant	[PMID: 38198520]

In Vitro

Upon oral administration, protein kinase C inhibitor Darovasertib (LXS196) binds to and inhibits PKC, which prevents the activation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest and apoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain types of cancer cells, is involved in tumor cell differentiation, proliferation, invasion and survival^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Darovasertib (LXS196; compound 9) (15, 30, 75, 150 mg/kg, P.O., mice) shows improved efficacy (regression) in a 92.1 GNAQ uveal melanoma xenograft model in a dose-dependently manner^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice implanted with 92.1 GNAQ mutant uveal melanoma cells^[2].
Dosage:	15, 30, 75, 150 mg/kg
Administration:	P.O. (bid) for 35 days
Result:	Dose-dependently suppressed the tumor growth.

Clinical Trial

분자량

472.47

화학식

C₂₂H₂₃F₃N₈O

CAS No.

1874276-76-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=C(C(NC2=C(N3CCC(C)(N)CC3)C=CC=N2)=O)N=C(C4=NC=CC=C4C(F)(F)F)C=N1

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

In Vitro:

DMSO : 25 mg/mL (52.91 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	2.1165 mL	10.5827 mL	21.1654 mL
5 mM	0.4233 mL	2.1165 mL	4.2331 mL
10 mM	0.2117 mL	1.0583 mL	2.1165 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기
농도 희석 계산기

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: ≥ 2.5 mg/mL (5.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 1.67 mg/mL (3.53 mM); Clear solution
Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (3.53 mM); Clear solution
Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.33 mg/mL (0.70 mM); Suspended solution; Need ultrasonic

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).

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.

순도&문서

Purity: 99.78%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (255 KB) HNMR (277 KB) RP-HPLC (232 KB) LCMS (330 KB)

Handling Instructions (2659 KB)

References

[1]. Protein Kinase C Inhibitor LXS196

[2]. US20180179181.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1165 mL	10.5827 mL	21.1654 mL	52.9134 mL
	5 mM	0.4233 mL	2.1165 mL	4.2331 mL	10.5827 mL
	10 mM	0.2117 mL	1.0583 mL	2.1165 mL	5.2913 mL
	15 mM	0.1411 mL	0.7055 mL	1.4110 mL	3.5276 mL
	20 mM	0.1058 mL	0.5291 mL	1.0583 mL	2.6457 mL
	25 mM	0.0847 mL	0.4233 mL	0.8466 mL	2.1165 mL
	30 mM	0.0706 mL	0.3528 mL	0.7055 mL	1.7638 mL
	40 mM	0.0529 mL	0.2646 mL	0.5291 mL	1.3228 mL
	50 mM	0.0423 mL	0.2117 mL	0.4233 mL	1.0583 mL

Darovasertib 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:

Darovasertib1874276-76-2LXS196 IDE196LXS 196LXS-196IDE196IDE 196IDE-196PKCProtein kinase CInhibitorinhibitorinhibit

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Darovasertib (Synonyms: LXS196; IDE196)

고객리뷰

Darovasertib Related Antibodies

4 Publications Citing Use of MCE Darovasertib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PKC Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

Darovasertib Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Darovasertib Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report