2. PROTAC MAPK/ERK Pathway GPCR/G Protein
  3. PROTACs Ras
  4. 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 ligase ligand (HY-170353); Black: linker (HY-176491);

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

PROTAC pan-KRAS degrader-1 Chemical Structure

PROTAC pan-KRAS degrader-1 Chemical Structure

CAS No. : 3043908-63-7

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PROTAC pan-KRAS degrader-1 Related Antibodies

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Description

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[1]. Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);

IC50 & Target

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)

In Vitro

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.

PROTAC pan-KRAS degrader-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: AGS, SW620, AsPC-1, H358, HCT116, MKN-1 cells
Concentration: 0.31, 1.22, 4.88, 19.53, 78.13, 312.5, 1250, 5000, 20000 nM
Incubation Time: 96 h
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.

Western Blot Analysis[1]

Cell Line: AGS, SW620 cells
Concentration: 0.16, 0.8, 4, 20, 100 nM
Incubation Time: 24 h
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.
Parmacokinetics
Species Dose Route Indicator value
Dog 1 mg/kg i.v. CL 6.19 mL/min/kg
Dog 1 mg/kg i.v. T1/2 20.5 hr
Dog 1 mg/kg i.v. Vss 3.46 L/kg
Dog 1 mg/kg i.v. AUClast 2522 ng·h/mL
Dog 1 mg/kg i.v. C0 9889 ng/mL
Molecular Weight

1192.38

Formula

C63H71F2N13O7S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC pan-KRAS degrader-1 Related Classifications

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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.

Keywords:

PROTAC pan-KRAS degrader-13043908-63-7PROTACsRasPROTACDegradationPan-KRASG12DG12CG12Vand G13DCancerInhibitorinhibitorinhibit

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