2. GPCR/G Protein MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. Ras PERK
  4. Elisrasib

Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRASG12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice.

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Elisrasib

Elisrasib Chemical Structure

CAS No. : 2914919-85-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Elisrasib Related Antibodies

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K-Ras H-Ras N-Ras Ras

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Description

Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRASG12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice[1].

In Vitro

Elisrasib (2-5 days) inhibits the proliferation of MIA-PA-CA-2 and NCI-H358 cells harboring the KRASG12C mutation with IC50 values of 0.44 nM and 0.6 nM[1], respectively.

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

Elisrasib Related Antibodies
Parmacokinetics
Species Dose Route Tmax AUC0-last F Cmax T1/2 Vdss CL
Mice[1] 10.3 mg/kg p.o. 1.0 h 1422 nM·h 21.9 % 431 nM / / /
Mice[1] 2.0 mg/kg i.v. / 1297 nM·h / / 1.7 h 3.9 L/kg 40.6 mL/min/kg
Rat[1] 2 mg/kg i.v. / 653 nM·h / / 1.9 h 10.6 L/kg 71.5 mL/min/kg
Rat[1] 9.8 mg/kg p.o. 1.5 h 995 nM·h 30.5 % 220 nM / / /
In Vivo

Elisrasib (10-30 mg/kg; oral administration; 22 days) has antitumor activity in a mouse model of pancreatic cancer[1].

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

Animal Model: Balb/c Nude treated Mia PaCa-2 cells[1]
Dosage: 10 and 30 mg/kg
Administration: oral administration; 22 days
Result: Inhibited the tumor volumes, with TGI of 93.06% and 99.64% by 10 mg/kg and 30 mg/kg, respectively.
Clinical Trial
Molecular Weight

679.66

Formula

C32H35F6N7O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)C(C(C)=CC(N)=C1F)=C1[C@@H]2CC3=NC(OC[C@@]45N(CCC5)C[C@@H](C4)F)=NC(N6C[C@@H](N(CC6)C(C(F)=C)=O)CC#N)=C3CO2
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 (147.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4713 mL 7.3566 mL 14.7132 mL
5 mM 0.2943 mL 1.4713 mL 2.9426 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (3.68 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% Corn Oil

    Solubility: 2.5 mg/mL (3.68 mM); Suspended solution; Need ultrasonic

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

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 1.4713 mL 7.3566 mL 14.7132 mL 36.7831 mL
5 mM 0.2943 mL 1.4713 mL 2.9426 mL 7.3566 mL
10 mM 0.1471 mL 0.7357 mL 1.4713 mL 3.6783 mL
15 mM 0.0981 mL 0.4904 mL 0.9809 mL 2.4522 mL
20 mM 0.0736 mL 0.3678 mL 0.7357 mL 1.8392 mL
25 mM 0.0589 mL 0.2943 mL 0.5885 mL 1.4713 mL
30 mM 0.0490 mL 0.2452 mL 0.4904 mL 1.2261 mL
40 mM 0.0368 mL 0.1839 mL 0.3678 mL 0.9196 mL
50 mM 0.0294 mL 0.1471 mL 0.2943 mL 0.7357 mL
60 mM 0.0245 mL 0.1226 mL 0.2452 mL 0.6131 mL
80 mM 0.0184 mL 0.0920 mL 0.1839 mL 0.4598 mL
100 mM 0.0147 mL 0.0736 mL 0.1471 mL 0.3678 mL
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Elisrasib 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:

Elisrasib2914919-85-8D3S-001RasPERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseMIA-PA-CA-2NCI-H358CD-1 mouseSprague-Dawley ratorally activeInhibitorinhibitorinhibit

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