1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. ADT-007

ADT-007 is a potent and orally active pan-RAS inhibitor with strong anticancer effects. ADT-007 binds RAS in a nucleotide-free conformation to block GTP activation. ADT-007 potently and selectively inhibits the growth of cancer cells with mutated or hyper-activated wild-type RAS isozymes.

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

ADT-007 Chemical Structure

ADT-007 Chemical Structure

CAS No. : 1945941-09-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 594 In-stock
Solution
10 mM * 1 mL in DMSO USD 594 In-stock
Solid
5 mg USD 540 In-stock
10 mg USD 950 In-stock
25 mg USD 1650 In-stock
50 mg USD 2700 In-stock
100 mg USD 4200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

ADT-007 is a potent and orally active pan-RAS inhibitor with strong anticancer effects. ADT-007 binds RAS in a nucleotide-free conformation to block GTP activation. ADT-007 potently and selectively inhibits the growth of cancer cells with mutated or hyper-activated wild-type RAS isozymes[1].

In Vitro

ADT-007 displays the highest potency and selectivity to inhibit the growth of KRASG13D HCT-116 cells with an IC50 of 5 nM, while RAS 110 wild-type HT-29 cells are ~100 fold less sensitive with an IC50 of 493 nM. ADT-007 displays even greater potency in KRAS G12C MIA PaCa-2 PDA cells, resulting in IC50 values as low as 2 nM. ADT-007 also potently inhibits the growth of three other mutant KRAS PDA cell lines with G12V or G12D mutations[1].

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

In Vivo

ADT-007 (10 mg/kg; intra-tumoral injection; once a day; for 17-21 days) strongly inhibits tumor growth in syngeneic immune competent mouse models of colorectal cancer[1].

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

Animal Model: 6-8-week-old BALB/C mice injected with colorectal cancer cells[1]
Dosage: 10 mg/kg
Administration: intra-tumoral injection; once a day; for 17-21 days
Result: Strongly inhibited tumor growth.
Molecular Weight

449.47

Formula

C26H24FNO5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCC1=CC=CO1)CC2=C(C)/C(C3=CC=C(F)C=C32)=C/C4=CC(OC)=C(C(OC)=C4)O

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 : 125 mg/mL (278.11 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 2.2248 mL 11.1242 mL 22.2484 mL
5 mM 0.4450 mL 2.2248 mL 4.4497 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

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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: 6.25 mg/mL (13.91 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    This protocol yields a clear solution of 6.25 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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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 2.2248 mL 11.1242 mL 22.2484 mL 55.6211 mL
5 mM 0.4450 mL 2.2248 mL 4.4497 mL 11.1242 mL
10 mM 0.2225 mL 1.1124 mL 2.2248 mL 5.5621 mL
15 mM 0.1483 mL 0.7416 mL 1.4832 mL 3.7081 mL
20 mM 0.1112 mL 0.5562 mL 1.1124 mL 2.7811 mL
25 mM 0.0890 mL 0.4450 mL 0.8899 mL 2.2248 mL
30 mM 0.0742 mL 0.3708 mL 0.7416 mL 1.8540 mL
40 mM 0.0556 mL 0.2781 mL 0.5562 mL 1.3905 mL
50 mM 0.0445 mL 0.2225 mL 0.4450 mL 1.1124 mL
60 mM 0.0371 mL 0.1854 mL 0.3708 mL 0.9270 mL
80 mM 0.0278 mL 0.1391 mL 0.2781 mL 0.6953 mL
100 mM 0.0222 mL 0.1112 mL 0.2225 mL 0.5562 mL
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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.

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ADT-007
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HY-157887
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