2. MAPK/ERK Pathway Stem Cell/Wnt
  3. ERK
  4. SHR2415

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.

For research use only. We do not sell to patients.

SHR2415 Chemical Structure

SHR2415 Chemical Structure

CAS No. : 2494010-42-1

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1 mg USD 362 In-stock
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25 mg USD 2799 In-stock
50 mg USD 4478 In-stock
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Based on 1 publication(s) in Google Scholar

SHR2415 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1].

IC50 & Target[1]

ERK1

2.8 nM (IC50)

ERK2

5.9 nM (IC50)

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.

SHR2415 Related Antibodies
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
Cmax(ng/mL) 604 219 526
AUC0-tp.o. (ng/mL•h) 2460 726 3271
t1/2p.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(%)
Cmax
(ng/mL)		 AUC
(h*ng/mL)		 Cmax
(ng/mL)		 AUC
(h*ng/mL)
SHR2415@25 mg/kg 5147 21364 9460 30260 1.42 112
Molecular Weight

463.92

Formula

C23H22ClN7O2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1555 mL 10.7777 mL 21.5554 mL
5 mM 0.4311 mL 2.1555 mL 4.3111 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. 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (5.39 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.

    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 (5.39 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
Purity & Documentation
References

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. 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 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:

SHR24152494010-42-1SHR 2415SHR-2415ERKExtracellular signal regulated kinasesERK1/2 kinaseRAS-RAF-MEK-ERK signaling pathwayoralERK1ERK2Colo205 cellscancerInhibitorinhibitorinhibit

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