2. PROTAC GPCR/G Protein MAPK/ERK Pathway Apoptosis
  3. PROTACs Ras Apoptosis
  4. CH091138

CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRASWT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the study of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand(HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)).

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CH091138 Chemical Structure

CH091138 Chemical Structure

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CH091138 Related Antibodies

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Description

CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRASWT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the study of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand(HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B))[1].

IC50 & Target[1]

KRas G12C

 

KRas G12D

 

KRas G12V

 

NEP108

3.8 μM (DC50)

In Vitro

CH091138 (0-30 μM, 24 h) blocks KRAS downstream signaling in cells harboring KRASG12D in AsPC1 cells[1].
CH091138 (0.01-100 μM, 3 days) exhibits a GI50 of 0.75 μM in KRASG12D mutant AsPC1 cells[1].
CH091138 (1-30 μM, 24 h) suppresses migration and invasion of AsPC-1[1].
CH091138 (1-10 μM, 24 h-21 d) is capable of suppressing colony formation and induces apoptosis of AsPC-1[1].
CH091138 (0-100 μM, 5 days) suppresses the growth of patient-derived organoids (PDOs) harboring KRASG12D more strongly than those with wild-type KRAS[1].

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

CH091138 Related Antibodies

Western Blot Analysis[1]

Cell Line: AsPC1-cells
Concentration: 0, 10, 30 μM
Incubation Time: 24 h
Result: Effectively inhibited KRAS-dependent downstream pathways p-AKT, p-MEK and p-ERK1/2 level.
Had no effect on other KRAS mutant cells.

Cell Viability Assay[1]

Cell Line: Patient-derived organoids (PDOs) with wild-type KRAS (COL-032-T and COL-047-T) and KRASG12D mutation (COL-018-T and COL-049-T)
Concentration: 0, 16.7 and 50 μM
Incubation Time: 5 days
Result: Exhibited an IC50 of 12.62-33.13 μM for KRASG12D PDO.
Exhibited an IC50 >50 μM for KRASWT PDO.
In Vivo

CH091138 (60 mg/kg , i.p., once every three days for 29 days) has a remarkable in vivo anti-tumoral activity with little weight change in the AsPC-1 xenograft model[1].

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

Animal Model: Xenograft model bearing AsPC-1 cells established in five-week-old female Balb/C nude mice[1]
Dosage: 60 mg/kg
Administration: Intraperitoneal injection (i.p.) once every three days for 29 days
Result: Achieved 61.8 % tumor growth inhibition.
Significantly decreased the average tumor weight and size.
Caused a decrease in KRAS level by up to 76.04 %.
Molecular Weight

1065.31

Formula

C59H69FN10O6S
SMILES

OC1=CC(C=CC=C2C#C)=C2C(C3=C(F)C(N=C(OC[C@@H]4CCCN4CCCCCCC(N[C@H](C(N5[C@H](C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@@H](O)C5)=O)C(C)(C)C)=O)N=C8N9C[C@H]%10N[C@H](CC%10)C9)=C8C=N3)=C1
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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CH091138 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:

CH091138CH 091138CH-091138PROTACsRasApoptosisKRASSelective KRAS G12D degraderMutant selectiveTargeted protein degradationVHL PROTACPancreatic cancerInhibitorinhibitorinhibit

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