2. PROTAC GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt
  3. PROTACs Ras ERK
  4. PROTAC KRAS G12D degrader 1

PROTAC KRAS G12D degrader 1 is a selective PROTAC KRASG12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRASG12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRASG12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893)).

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

PROTAC KRAS G12D degrader 1

PROTAC KRAS G12D degrader 1 Chemical Structure

CAS No. : 3033583-54-6

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Based on 1 publication(s) in Google Scholar

PROTAC KRAS G12D degrader 1 Related Antibodies

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Description

PROTAC KRAS G12D degrader 1 is a selective PROTAC KRASG12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRASG12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRASG12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893))[1].

IC50 & Target[1]

VHL

 

KRas G12D

 

In Vitro

PROTAC KRAS G12D degrader 1 (Compound 8o) (24 h) dose-dependently degrades KRASG12D in SNU-1, HPAF-II, AGS, and PANC 04.03 cells (heterozygous KRASG12D) with DC50 values of 19.77 nM, 52.96 nM, 7.49 nM, and 87.8 nM, respectively[1].
PROTAC KRAS G12D degrader 1 (1 μM, 1-24 h) significantly decreases KRASG12D protein level in AsPC-1 cells[1].
PROTAC KRAS G12D degrader 15 days) inhibits the proliferation of KRASG12D mutant cells including AsPC-1, SNU-1, HPAF-II, AGS, and PANC 04.03 with IC50 values of 59.97 nM, 43.51 nM, 31.36 nM, 51.53 nM, and >10000 nM, respectively[1].
PROTAC KRAS G12D degrader 1 (1 μM, 6 h) leads to sustained KRASG12D degradation and pERK inhibition in AsPC-1 cells[1].

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

PROTAC KRAS G12D degrader 1 Related Antibodies
In Vivo

PROTAC KRAS G12D degrader 1 (Compound 8o) (50 mg/kg, s.c., once daily or every three days, 22 days) inhibits tumor growth in BALB/c nude mice bearing AsPC-1 xenografts[1].

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

Animal Model: AsPC-1 cells (5 × 106 in 100 µL) were subcutaneously implanted into the flanks of 8-9-week-old BALB/c nude mice[1]
Dosage: 50 mg/kg
Administration: s.c., once daily or every three days, 22 days
Result: Achieved tumor growth inhibition.
Reduced KRASG12D protein level and the phosphorylation level of ERK in AsPC-1 xenograft tumor tissues.
Downregulated the mRNA level of DUSP4.
Showed no significant changes in body weight.
Molecular Weight

1103.33

Formula

C59H72F2N10O7S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=C(CC)C2=C(C3=NC=C4C(N=C(OC[C@@H]5CCCN5CCCCOCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(N[C@@H](C)C7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)N=C4N9C[C@H]%10N[C@H](CC%10)C9)=C3F)C=C(O)C=C2C=C1
Shipping

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

DMSO : 10 mg/mL (9.06 mM; ultrasonic and warming and heat to 60°C; 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 0.9063 mL 4.5317 mL 9.0635 mL
5 mM 0.1813 mL 0.9063 mL 1.8127 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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Purity & Documentation

Purity: 98.32%

SDS (251 KB)

COA (247 KB) HNMR (335 KB) RP-HPLC (169 KB) LCMS (234 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 0.9063 mL 4.5317 mL 9.0635 mL 22.6587 mL
5 mM 0.1813 mL 0.9063 mL 1.8127 mL 4.5317 mL
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PROTAC KRAS G12D degrader 1 Related Classifications

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  • 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:

PROTAC KRAS G12D degrader 13033583-54-6PROTACsRasERKExtracellular signal regulated kinasesPROTACAsPC-1HPAF-IIPANCInhibitorinhibitorinhibit

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