PROTAC pan-KRAS degrader-1
PROTAC pan-KRAS degrader-1 is a pan-KRAS PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc.
(Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligand (HY-170353); Black: linker (HY-176491)).
For research use only. We do not sell to patients.
- CAS No.: 3043908-63-7
- Formula: C63H71F2N13O7S
- Molecular Weight:1192.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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KRas G12D 1.1 nM (DC50) |
KRas G12D 3 nM (IC50) |
KRAS(G12C) 5 nM (IC50) |
KRas G12V 10 nM (IC50) |
KRas G12D 2.6 nM (IC50) |
KRAS G13D 13 nM (IC50) |
PROTAC pan-KRAS degrader-1 (Compound 144) (0.31-20000 nM, 96 h) significantly inhibits cell proliferation with different KRAS mutation types in AGS, SW620, AsPC-1, H358, HCT116, MKN-1 cells, with IC50 s of 3, 10, 2.6, 5, 13, and 0.9 nM, respectively[1].
PROTAC pan-KRAS degrader-1 (1.53-100000 nM) potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%[1].
PROTAC pan-KRAS degrader-1 (0.16-100 nM, 24 h) potently degrades different KRAS mutation (G12D and G12V) in AGS and SW620 cells, with the maximum degradation efficacy at 0.8 and 4 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AGS, SW620, AsPC-1, H358, HCT116, MKN-1 cells
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Concentration:0.31, 1.22, 4.88, 19.53, 78.13, 312.5, 1250, 5000, 20000 nM
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Incubation Time:96 h
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Result:Significantly inhibited cell proliferation with different KRAS mutation types in AGS (G12D), SW620 (G12V), AsPC-1 (G12D), H358 (G12C), HCT116 (G13D), MKN-1 cells (WT amp), with IC50 s of 3, 10, 2.6, 5, 13, and 0.9 nM, respectively.
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Cell Line:AGS, SW620 cells
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Concentration:0.16, 0.8, 4, 20, 100 nM
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Incubation Time:24 h
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Result:Potently degraded different KRAS mutation (G12D and G12V) in AGS and SW620 cells, and the maximum degradation efficacy at 0.8 and 4 nM, respectively.
| Species | Dose | Route | CL | T1/2 | Vss | AUClast | C0 |
|---|---|---|---|---|---|---|---|
| Dog | 1 mg/kg | i.v. | 6.19 mL/min/kg | 20.5 h | 3.46 L/kg | 2522 ng·h/mL | 9889 ng/mL |
Chemical Information
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CAS No. 3043908-63-7
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Molecular Weight 1192.38
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Formula C63H71F2N13O7S
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SMILES
FC(C=C1)=C(CC)C(C1=CC(O)=C2)=C2C3=NC=C4C(N=C(OCC5(CC5)CN6CCC(OC7=NC=C(C8=CN([C@@H](C(C)C)C(N9C[C@H](O)C[C@H]9C(N[C@@H](C)C%10=CC=C(C%11=C(C)N=CS%11)C=C%10)=O)=O)N=N8)N=C7)CC6)N=C4N%12CCC[C@@](C)(O)C%12)=C3F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC pan-KRAS degrader-1 Related Classifications
HY-176489 Related Classifications
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