Art. -Nr.: HY-151367

SHR2415

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SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC₅₀ values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC₅₀ value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer.

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Reinheit: 98.04%
CAS. Nr.: 2494010-42-1
Formel: C₂₃H₂₂ClN₇O₂
Molecular Weight:463.92

Speicherung:

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

SHR2415 Chemical Structure

CAS. Nr.: 2494010-42-1

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ERK1

2.8 nM (IC₅₀)

ERK2

5.9 nM (IC₅₀)

Alle ERK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	44.6 nM Compound: 8; SHR2415	Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability for 72 hrs by cell titre glo luminescence assay	[PMID: 35450372]

In Vitro

SHR2415 has inhibition activity for ERK1 and ERK2 with IC₅₀ values of 2.8 nM and 5.9 nM, respectively^[1].
SHR2415 shows the cellular potency with an IC₅₀ value of 44.6 nM in Colo205 cells^[1].

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

In Vivo

SHR2415 (i.v. (1 mg/kg for mouse and rat) and p.o. (2 mg/kg for mouse, rat, and dog)) displays a favorable PK profile across species with low clearance and good in vivo exposure^[1].
SHR2415 (25, 50 mg/kg; p.o.; once daily, for 14 days) displays favorable PK profiles across species as well as robust in vivo efficacy in a mouse Colo205 xenograft model^[1].

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

Animal Model:

Mouse, Rat and Dog^[1]
Dosage:

1 mg/kg (mouse and rat), 0.5 mg/kg (dog), 2 mg/kg (mouse, rat, and dog)
Administration:

i.v. (mouse and rat) and p.o. (mouse, rat, and dog)

Result:

Species	Mouse	Rat	Dog
C_max(ng/mL)	604	219	526
AUC_0-tp.o. (ng/mL•h)	2460	726	3271
t_1/2p.o. (h)	3.5	2.1	3.2
CL(mL/min/kg)	12.2	25.3	10.5
F (%)	90.8	45.8	101

Animal Model:

Balb/c mouse Colo205 tumor xenograft model^[1]
Dosage:

25, 50 mg/kg
Administration:

p.o.; once daily, for 14 days

Result:

Cpds ID @ Dose	Plasma		Tumor		AUC-tumor/AUC-plasma	TGI(%)
	C_max (ng/mL)	AUC (h*ng/mL)	C_max (ng/mL)	AUC (h*ng/mL)
SHR2415@25 mg/kg	5147	21364	9460	30260	1.42	112

Chemical Information

CAS. Nr. 2494010-42-1
Appearance Solid
Molecular Weight 463.92
Formel C₂₃H₂₂ClN₇O₂
Color Off-white to light yellow
SMILES

CC1=CN=C(N=C1C2=CN3C(N(CC3=C2)[C@@H](C4=CC(Cl)=CC=C4)CO)=O)NC5=CC=NN5C
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 (215.55 mM; Need ultrasonic; 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

2.1555 mL

10.7777 mL

21.5554 mL

5 mM

0.4311 mL

2.1555 mL

4.3111 mL

10 mM

0.2156 mL

1.0778 mL

2.1555 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 (5.39 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.39 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.39 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 (278 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]. Xin Li, et al. Discovery of SHR2415, a Novel Pyrrole-Fused Urea Scaffold ERK1/2 Inhibitor. ACS Med Chem Lett. 2022 Apr 1;13(4):701-706. [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	2.1555 mL	10.7777 mL	21.5554 mL	53.8886 mL
	5 mM	0.4311 mL	2.1555 mL	4.3111 mL	10.7777 mL
	10 mM	0.2156 mL	1.0778 mL	2.1555 mL	5.3889 mL
	15 mM	0.1437 mL	0.7185 mL	1.4370 mL	3.5926 mL
	20 mM	0.1078 mL	0.5389 mL	1.0778 mL	2.6944 mL
	25 mM	0.0862 mL	0.4311 mL	0.8622 mL	2.1555 mL
	30 mM	0.0719 mL	0.3593 mL	0.7185 mL	1.7963 mL
	40 mM	0.0539 mL	0.2694 mL	0.5389 mL	1.3472 mL
	50 mM	0.0431 mL	0.2156 mL	0.4311 mL	1.0778 mL
	60 mM	0.0359 mL	0.1796 mL	0.3593 mL	0.8981 mL
	80 mM	0.0269 mL	0.1347 mL	0.2694 mL	0.6736 mL
	100 mM	0.0216 mL	0.1078 mL	0.2156 mL	0.5389 mL

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SHR2415

MCE Bioactive Compound Library

Alle ERK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SHR2415 Related Classifications

HY-151367 Related Classifications