PROTAC KRAS G12D degrader 1
Based on 1 Customer Validation
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)).
(Pink: KRas G12D Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.32%
- CAS No.: 3033583-54-6
- Formula: C59H72F2N10O7S
- Molecular Weight:1103.33
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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VHL |
KRas G12D |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AGS | IC50 |
31.36 nM
Compound: 8o
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Antiproliferative activity against human AGS cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human AGS cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
|
[PMID: 38197882] |
| ASPC1 | IC50 |
231.2 nM
Compound: 8o
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Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability incubated for 6 hrs followed by compound washout measured after 114 hrs by Cell Titer Glo assay
Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability incubated for 6 hrs followed by compound washout measured after 114 hrs by Cell Titer Glo assay
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[PMID: 38197882] |
| ASPC1 | IC50 |
59.97 nM
Compound: 8o
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Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
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[PMID: 38197882] |
| ASPC1 | IC50 |
61.14 nM
Compound: 8o
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Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability incubated for 120 hrs of continuous treatment by Cell Titer Glo assay
Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability incubated for 120 hrs of continuous treatment by Cell Titer Glo assay
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[PMID: 38197882] |
| HPAF-II | IC50 |
45.22 nM
Compound: 8o
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Antiproliferative activity against human HPAF-II cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human HPAF-II cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
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[PMID: 38197882] |
| NCI-H1975 | IC50 |
>10000 nM
Compound: 8o
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Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
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[PMID: 38197882] |
| NCI-H358 | IC50 |
>9000 nM
Compound: 8o
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Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
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[PMID: 38197882] |
| SNU1 | IC50 |
43.51 nM
Compound: 8o
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Antiproliferative activity against human SNU1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
Antiproliferative activity against human SNU1 cells harboring KRAS G12D mutant assessed as inhibition of cell viability incubated for 5 days by Cell Titer Glo assay
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[PMID: 38197882] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:50 mg/kg
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Administration:s.c., once daily or every three days, 22 days
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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.
Chemical Information
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CAS No. 3033583-54-6
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Appearance Solid
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Molecular Weight 1103.33
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Formula C59H72F2N10O7S
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Color Off-white to light yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 |
PROTAC KRAS G12D degrader 1 Related Classifications
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