2. PROTAC GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt PI3K/Akt/mTOR
  3. PROTACs Ras ERK Akt
  4. Setidegrasib

Setidegrasib  (Synonyms: ASP-3082; KRAS G12D inhibitor 17)

Cat. No.: HY-148273 Purity: 99.42%
COA
SDS
Handling Instructions Technical Support

Setidegrasib (KRAS G12D inhibitor 17, ASP3082) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses p-ERK, p-AKT, p-S6 levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used for the study of KRAS(G12D)-mutated solid tumors. (Blue: VHL ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)).

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

Setidegrasib

Setidegrasib Chemical Structure

CAS No. : 2821793-99-9

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Based on 1 publication(s) in Google Scholar

Setidegrasib Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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K-Ras H-Ras N-Ras Ras

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ERK ERK1 ERK2 ERK5 ERK8

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Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Setidegrasib (KRAS G12D inhibitor 17, ASP3082) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses p-ERK, p-AKT, p-S6 levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used for the study of KRAS(G12D)-mutated solid tumors. (Blue: VHL ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700))[1][2].

IC50 & Target[1][2]

KRAS(G12D)

37 nM (DC50)

VHL

 

In Vitro

Setidegrasib (24 h) inhibits ERK phosphorylation in human G12D-mutant KRAS-positive pancreatic cancer strain AsPC-1, with an IC50 of 15 nM[1].
Setidegrasib (6 days) inhibits anchorage-independent cell growth against human G12D-mutant KRAS-positive pancreatic cancer strain AsPC-1, with an IC50 of 23 nM[1].
Setidegrasib (6 days) potently inhibits proliferation of multiple KRAS(G12D)-mutated cancer cell lines (PK-59, HPAC, GP2d, GP5d) in 3D assay, while showing weak activity (IC50 > 10 μM) against KRAS(WT) cells (A375, HT-29) and other KRAS mutants (G12V, G12C, G13D) via CellTiter-Glo assay[2].
Setidegrasib (1 μM, 4-24 h) selectively reduces KRAS(G12D) and DUSP4 (a MAPK-dependent gene) levels in AsPC-1 cells[2].
Setidegrasib (30-300 nM, 6-72 h) sustains KRAS(G12D) degradation (including GTP-bound form) and suppresses p-ERK, p-AKT, p-S6 levels in AsPC-1 cells[2].

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

Setidegrasib Related Antibodies

Western Blot Analysis[2]

Cell Line: AsPC-1 cells
Concentration: 30, 100, 300 nM
Incubation Time: 6, 24, 48, 72 h
Result: Sustained KRAS(G12D) degradation (including GTP-bound form).
Suppressed p-ERK, p-AKT, p-S6 levels in AsPC-1 cells.
In Vivo

Setidegrasib (0.3-30 mg/kg, i.v., once/twice weekly, 14-22 days) exhibits dose-dependent anti-tumor activity in PK-59, LXFA 1125 NSCLC PDX, AsPC-1 (pancreatic) and GP2d (colorectal) KRAS(G12D)-mutated xenograft models of Balb/c nu/nu nude mice[1][2].

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

Animal Model: PK-59, AsPC-1, HPAC, PK-1, GP2d, GP5d, A375, KP-4, and HT-29 cells were subcutaneously inoculated into the flank of 4-8 week-old male nude mice (Balb/c nu/nu) at 1-6 × 106 cells per 0.1–0.2 ml(Matrigel (Corning):PBS = 1:1)/mouse[2]
Dosage: 0.3, 1, 3, 10, 30 mg/kg
Administration: i.v., once/twice weekly, 14, 21, 22 days
Result: Achieved tumor growth inhibition in PK-59, LXFA 1125 NSCLC PDX, AsPC-1 (pancreatic) and GP2d (colorectal) KRAS(G12D)-mutated xenograft models of Balb/c nu/nu nude mice.
Showed no significant changes in body weight.
Showed no significant tumor growth inhibition in A375 (melanoma) and HT-29 (colorectal) KRAS(WT) xenograft models.
Molecular Weight

1117.30

Formula

C60H65FN12O7S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)C)N4C=C(N=N4)C5=CC=C(C=C5)COC6=[C@]([C@]7=C(C(F)=CC8=C7C=NN8)C)C(C9CC9)=CC%10=C6N=C(N=C%10N%11C[C@@H]%12C[C@H]%11CN%12)OC%13CCOCC%13)=O)O)=O)CO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (89.50 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 0.8950 mL 4.4751 mL 8.9501 mL
5 mM 0.1790 mL 0.8950 mL 1.7900 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 (protect from light). 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (2.24 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.65%

SDS (252 KB)

COA (262 KB) HNMR (228 KB) RP-HPLC (118 KB) LCMS (145 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 (protect from light). 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 0.8950 mL 4.4751 mL 8.9501 mL 22.3754 mL
5 mM 0.1790 mL 0.8950 mL 1.7900 mL 4.4751 mL
10 mM 0.0895 mL 0.4475 mL 0.8950 mL 2.2375 mL
15 mM 0.0597 mL 0.2983 mL 0.5967 mL 1.4917 mL
20 mM 0.0448 mL 0.2238 mL 0.4475 mL 1.1188 mL
25 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
30 mM 0.0298 mL 0.1492 mL 0.2983 mL 0.7458 mL
40 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5594 mL
50 mM 0.0179 mL 0.0895 mL 0.1790 mL 0.4475 mL
60 mM 0.0149 mL 0.0746 mL 0.1492 mL 0.3729 mL
80 mM 0.0112 mL 0.0559 mL 0.1119 mL 0.2797 mL
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Setidegrasib 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:

Setidegrasib2821793-99-9ASP-3082 KRAS G12D inhibitor 17ASP3082ASP 3082PROTACsRasERKAktExtracellular signal regulated kinasesPKBProtein kinase BPROTAC compoundprotein degradationG12D-mutationInhibitorinhibitorinhibit

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