Art. -Nr.: HY-144269

SHR902275

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SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC₅₀s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF^wt, and bRAF^V600E, respectively. SHR902275 shows cell growth inhibition with GI₅₀s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively.

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Reinheit: 99.80%
CAS. Nr.: 2695506-82-0
Formel: C₂₆H₂₃F₃N₄O₄
Molecular Weight:512.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SHR902275 Chemical Structure

CAS. Nr.: 2695506-82-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

C-Raf

1.6 nM (IC₅₀)

BRaf^V600E

5.7 nM (IC₅₀)

BRAF^WT

10 nM (IC₅₀)

Alle Raf Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	GI₅₀	0.17 μM Compound: 33; SHR902275	Cytotoxicity against human A-375 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay Cytotoxicity against human A-375 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay	[PMID: 34906761]
Calu-6	GI₅₀	0.4 μM Compound: 33; SHR902275	Cytotoxicity against human Calu-6 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay Cytotoxicity against human Calu-6 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay	[PMID: 34906761]
NCI-H358	GI₅₀	1.4 μM Compound: 33; SHR902275	Cytotoxicity against human NCI-H358 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay Cytotoxicity against human NCI-H358 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay	[PMID: 34906761]
SK-MEL-2	GI₅₀	0.32 μM Compound: 33; SHR902275	Cytotoxicity against human SK-MEL-2 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay Cytotoxicity against human SK-MEL-2 cells assessed as inhibition of growth measured after 72 hrs by CellTiter-Glo luciferase assay	[PMID: 34906761]

Chemical Information

CAS. Nr. 2695506-82-0
Appearance Solid
Molecular Weight 512.48
Formel C₂₆H₂₃F₃N₄O₄
Color White to off-white
SMILES

O=C(C1=NN=CC(C(F)(F)F)=C1)NC2=CC=C(C)C(C3=CC4=C(NC(CC5(CCOCC5)O4)=O)C=C3)=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (195.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9513 mL

9.7565 mL

19.5130 mL

5 mM

0.3903 mL

1.9513 mL

3.9026 mL

10 mM

0.1951 mL

0.9756 mL

1.9513 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (4.88 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.88 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhao P, et al. Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers. Eur J Med Chem. 2022;228:114040. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1.9513 mL	9.7565 mL	19.5130 mL	48.7824 mL
	5 mM	0.3903 mL	1.9513 mL	3.9026 mL	9.7565 mL
	10 mM	0.1951 mL	0.9756 mL	1.9513 mL	4.8782 mL
	15 mM	0.1301 mL	0.6504 mL	1.3009 mL	3.2522 mL
	20 mM	0.0976 mL	0.4878 mL	0.9756 mL	2.4391 mL
	25 mM	0.0781 mL	0.3903 mL	0.7805 mL	1.9513 mL
	30 mM	0.0650 mL	0.3252 mL	0.6504 mL	1.6261 mL
	40 mM	0.0488 mL	0.2439 mL	0.4878 mL	1.2196 mL
	50 mM	0.0390 mL	0.1951 mL	0.3903 mL	0.9756 mL
	60 mM	0.0325 mL	0.1626 mL	0.3252 mL	0.8130 mL
	80 mM	0.0244 mL	0.1220 mL	0.2439 mL	0.6098 mL
	100 mM	0.0195 mL	0.0976 mL	0.1951 mL	0.4878 mL

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SHR902275

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alle Raf Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SHR902275

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alle Raf Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SHR902275 Related Classifications

HY-144269 Related Classifications