FRAX597

Name: FRAX597
Brand: MedChemExpress
SKU: HY-15542A
Rating: 5.0 (9 reviews)

Cat. No.: HY-15542A Pureza: 99.36%: Ficha de datos
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FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC₅₀ of 8, 13 and 19 nM for PAK1, 2 and 3.

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FRAX597 Estructura química

No. CAS : 1286739-19-2

Tamaño	Stock	Cantidad

Muestra gratis (0.1 - 0.2 mg)	Solicite ahora
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	Obtener un presupuesto	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Revisión del cliente

Based on 9 publication(s) in Google Scholar

9 Publications Citing Use of MCE FRAX597

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas PAK:

Ver todas las isoformas

PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

Actividad biológica
Protocolo
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC₅₀ of 8, 13 and 19 nM for PAK1, 2 and 3.

IC₅₀ & Target^[1]

PAK1

8 nM (IC₅₀)

PAK2

13 nM (IC₅₀)

PAK3

19 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
MCF-10A	IC₅₀	0.088 3 Compound: FRAX-597	Inhibition of PAK1 phosphorylation in human MCF10A cells Inhibition of PAK1 phosphorylation in human MCF10A cells	[PMID: 27994749]
MCF-10A	IC₅₀	0.088 3 Compound: FRAX-597	Inhibition of PAK1 phosphorylation in human MCF10A cells Inhibition of PAK1 phosphorylation in human MCF10A cells	[PMID: 27994749]
MDA-MB-231	IC₅₀	4.16 3 Compound: FRAX597	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition	[PMID: 32738980]
MDA-MB-231	IC₅₀	4.16 3 Compound: FRAX597	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition	[PMID: 32738980]

In Vitro

FRAX597 is determined to be a potent, ATP-competitive inhibitor of group I PAKs (PAK 1-3), with biochemical IC₅₀ values as follows: PAK1 IC₅₀=8 nM, PAK2 IC₅₀=13 nM, PAK3 IC₅₀=19 nM. The IC₅₀ toward PAK4, a member of group II PAKs is >10 μM. At a concentration of 100 nM FRAX597 displays a significant (>80% inhibition) inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%). When measured using the Kinase Glo Assay in the presence of 20 nM protein and 1 μM ATP, FRAX597 displayed an IC₅₀ value of 48 nM against wild type PAK1, while IC₅₀ values against the V342F and V342Y PAK1 mutants are higher than 3 μM and 2 μM, respectively^[1].

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

In Vivo

Analysis of the flux reading for the animals in the two cohorts demonstrates a significantly slower tumor growth rate in FRAX597-treated mice compared with control mice. After 14 days of treatment the animals are sacrificed and the tumors excised and weighed. FRAX597-treated cohort shows significantly lower average tumor weight compared with the control cohort ^[1].

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

Peso molecular

558.10

Fòrmula

C₂₉H₂₈ClN₇OS

No. CAS

1286739-19-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(C2=CC=C(C3=CN=CS3)C=C2Cl)=CC4=CN=C(NC5=CC=C(N6CCN(C)CC6)C=C5)N=C4N1CC

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

In Vitro:

DMSO : 14.29 mg/mL (25.60 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	1.7918 mL	8.9590 mL	17.9179 mL
5 mM	0.3584 mL	1.7918 mL	3.5836 mL
10 mM	0.1792 mL	0.8959 mL	1.7918 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.

Calculadora de molaridad
Calculadora de dilución

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: 1.43 mg/mL (2.56 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.43 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: 1.43 mg/mL (2.56 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.43 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: ≥ 1.43 mg/mL (2.56 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 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 (14.3 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).

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.

Pureza y Documentación

Purity: 99.36%

Select Batch:

Ficha de datos (277 KB) SDS (393 KB)

COA (246 KB) LCMS (98 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Licciulli S, et al. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem. 2013 Oct 4;288(40):29105-14. [Content Brief]

Ensayo celular ^[1]	30,000 SC4 cells/well are plated in 12-well dishes in triplicate. Cell growth media with or without FRAX597 (1 μM) is replaced daily. At indicated time points, cells from individual wells are trypsinized and counted using a Coulter counter. Statistical analysis is performed using a Student's t test. For cell cycle analysis, cells are harvested, washed once with PBS and fixed in cold 70% ethanol. Fixed cells are resuspended in propidium iodide (PI) buffer (50 μg/mL PI, 250 mg/mL RNase A in PBS) and incubated overnight at 4°C in the dark. Cell cycle distribution is evaluated using Coulter Epics XL flow cytometer. Data are analyzed using WinMDI software^[1]. MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Administraciòn de animales ^[1]	Mice^[1] Nf2^-/- SC4 Schwann cells are transduced by lentiviruses carrying pLuc-mCherry and sorted by FACS. 5×10⁴ cells are transplanted into the sciatic nerve sheath of NOD/SCID mice (8 weeks of age) by intraneural injection. Tumor progression is monitored weekly by bioluminescence imaging (BLI) on an IVIS-200 system. The representative images from bioluminescence imaging (BLI) of mice carrying orthotopic tumors treated with FRAX597 (100 mg/kg) or vehicle control at day 14 of treatment. NOD/SCID mice are injected intraneurally with 5×10⁴ SC4/pLuc-mCherry cells and are enrolled into treatment after 10 days. Mice are treated daily for 14 days and imaged every 3 days to follow tumor development. MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias	[1]. Licciulli S, et al. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem. 2013 Oct 4;288(40):29105-14. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.7918 mL	8.9590 mL	17.9179 mL	44.7948 mL
	5 mM	0.3584 mL	1.7918 mL	3.5836 mL	8.9590 mL
	10 mM	0.1792 mL	0.8959 mL	1.7918 mL	4.4795 mL
	15 mM	0.1195 mL	0.5973 mL	1.1945 mL	2.9863 mL
	20 mM	0.0896 mL	0.4479 mL	0.8959 mL	2.2397 mL
	25 mM	0.0717 mL	0.3584 mL	0.7167 mL	1.7918 mL

FRAX597 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:

FRAX5971286739-19-2FRAX 597FRAX-597PAKp21 activated kinasesInhibitorinhibitorinhibit

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FRAX597

Revisión del cliente

FRAX597 Related Antibodies

9 Publications Citing Use of MCE FRAX597

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas PAK:

Actividad biológica

Protocolo

Pureza y Documentación

Referencias

Revisión del cliente

FRAX597 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

FRAX597 Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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