2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. Divarasib

Divarasib  (Synonyms: GDC-6036)

Cat. No.: HY-145928 Purity: 99.46%
COA Handling Instructions

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Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.

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

Divarasib Chemical Structure

Divarasib Chemical Structure

CAS No. : 2417987-45-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1026 In-stock
Solution
10 mM * 1 mL in DMSO USD 1026 In-stock
Solid
5 mg USD 750 In-stock
10 mg USD 1050 In-stock
25 mg USD 1890 In-stock
50 mg USD 2650 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Divarasib:

Divarasib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Divarasib

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K-Ras H-Ras Ras

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.

IC50 & Target[1]

K-Ras(G12C)

<0.01 μM (IC50)

In Vitro

Divarasib (compound 17a) has an EC50 of 2 nM in K-Ras G12C-alkylation HCC1171 cells[2]

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

Divarasib Related Antibodies
In Vivo

Divarasib (10-100 mg/kg/day; PO for 7 days) decreases the ratio of free KRAS G12C[1].

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

Animal Model: Female C.B-17 SCID (Inbred) mice (20-21 weeks old; 24.1 g) with human NSCLC NCI-H2030.X1.1 cells[1]
Dosage: 10, 25, or 100 mg/kg
Administration: Oral gavage (PO) every day (QD) for 7 days (vehicle: 0.5% methylcellulose)
Result: Decreased the ratio of free KRAS G12C to internal standard.
Dose-dependent target engagement was observed for all time points (2, 8, and 24 h post-last dose), with over 90% KRAS G12C engagement observed for the highest dose 100 mg/kg assessed.
Clinical Trial
Molecular Weight

622.06

Formula

C29H32ClF4N7O2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

NC1=N[C@]([C@]2=C(C=C3C(N=C(N=C3N4[C@H](CN(CC4)C(C=C)=O)C)OC[C@H]5N(CCC5)C)=C2F)Cl)=C(C(C)=C1)C(F)(F)F
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 (160.76 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 1.6076 mL 8.0378 mL 16.0756 mL
5 mM 0.3215 mL 1.6076 mL 3.2151 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 (4.02 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 (4.02 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 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

Purity: 99.46%

COA (252 KB) HNMR (318 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
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 1.6076 mL 8.0378 mL 16.0756 mL 40.1890 mL
5 mM 0.3215 mL 1.6076 mL 3.2151 mL 8.0378 mL
10 mM 0.1608 mL 0.8038 mL 1.6076 mL 4.0189 mL
15 mM 0.1072 mL 0.5359 mL 1.0717 mL 2.6793 mL
20 mM 0.0804 mL 0.4019 mL 0.8038 mL 2.0095 mL
25 mM 0.0643 mL 0.3215 mL 0.6430 mL 1.6076 mL
30 mM 0.0536 mL 0.2679 mL 0.5359 mL 1.3396 mL
40 mM 0.0402 mL 0.2009 mL 0.4019 mL 1.0047 mL
50 mM 0.0322 mL 0.1608 mL 0.3215 mL 0.8038 mL
60 mM 0.0268 mL 0.1340 mL 0.2679 mL 0.6698 mL
80 mM 0.0201 mL 0.1005 mL 0.2009 mL 0.5024 mL
100 mM 0.0161 mL 0.0804 mL 0.1608 mL 0.4019 mL
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Divarasib 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:

Divarasib2417987-45-0GDC-6036GDC6036GDC 6036RasK-Ras G12CHCC1171NSCLC NCI-H2030.X1.1 cell,Inhibitorinhibitorinhibit

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