2. PROTAC MAPK/ERK Pathway GPCR/G Protein Apoptosis Stem Cell/Wnt
  3. PROTACs Ras Caspase ERK
  4. PROTAC K-Ras Degrader-5

PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC50 of <100 nM for KRASG12D. PROTAC K-Ras Degrader-5 recruits KRASG12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses pERK levels downstream of KRASG12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer.
(Pink: K-RAS ligand (HY-168671); Blue: Cereblon E3 ligase ligand; Black: linker).

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

PROTAC K-Ras Degrader-5

PROTAC K-Ras Degrader-5 Chemical Structure

CAS No. : 3052745-16-8

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Customer Review

Based on 1 publication(s) in Google Scholar

PROTAC K-Ras Degrader-5 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

PROTAC K-Ras Degrader-5 is a cereblon-based K-Ras PROTAC degrader with a DC50 of <100 nM for KRASG12D. PROTAC K-Ras Degrader-5 recruits KRASG12D to the cereblon E3 ubiquitin ligase complex for ubiquitination and subsequent proteasomal degradation. PROTAC K-Ras Degrader-5 suppresses pERK levels downstream of KRASG12D degradation in cancer cells. PROTAC K-Ras Degrader-5 reduces proliferation of cancer cells. PROTAC K-Ras Degrader-5 induces caspase 3/7 activity and cPARP, markers of apoptosis, in pancreatic cancer spheroids and tumors. PROTAC K-Ras Degrader-5 can be used for the research of pancreatic cancer and colorectal cancer[1]. (Pink: K-RAS ligand (HY-168671); Blue: Cereblon E3 ligase ligand; Black: linker).

IC50 & Target

Cereblon

 

KRas G12D

<100 nM (DC50)

Caspase 3

 

Caspase-7

 

In Vitro

PROTAC K-Ras Degrader-5 (compound 69) (0.01-100 nM) inhibits the viability of AsPC-1, Panc04.03, SW1990, Panc08.13, LS180 and A427 cells[1].
PROTAC K-Ras Degrader-5 (0.01-1000 nM; 24-96 h) suppresses the level of pERK in AsPC-1 spheroids[1].
PROTAC K-Ras Degrader-5 (0.5-4 nM; 16 h) induces caspase 3/7 activity in pancreatic cancer spheroids[1].

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

PROTAC K-Ras Degrader-5 Related Antibodies
In Vivo

PROTAC K-Ras Degrader-5 (compound 69) (1-3 mg/kg; i.v.; twice weekly; once weekly; once every two weeks) effectively inhibits tumor growth in GP2d colorectal cancer mice, with all tumor inhibition rates exceeding 90%[1].
PROTAC K-Ras Degrader-5 AsPC-1 (0.3-3 mg/kg; i.v.; twice weekly; once weekly; once every two weeks) effectively inhibits tumor growth in AsPC-1, SW1990, HPAC and Panc04.03 pancreatic cancer xenograft mouse models[1].

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

Animal Model: CB17 SCID female mice (6-8 weeks old) were subcutaneously injected with GP2d colorectal cancer cells[1]
Dosage: 1 mg/kg, 3 mg/kg
Administration: i.v.; twice weekly; once weekly; once every two weeks
Result: Led to 93-102% tumor growth inhibition (TGI).
Molecular Weight

1025.17

Formula

C57H63F3N10O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

C#CC1=C(C=CC2=CC(O)=CC(C3=C(C4=NC(OCCN5CCC(CC5)CC6CCN(CC6)CC7CCN(CC7)C8=CC=C9C(N(CC9=C8F)C%10CCC(NC%10=O)=O)=O)=NC(N%11C[C@H]%12N[C@H](CC%12)C%11)=C4C=N3)F)=C21)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (97.54 mM; Need ultrasonic; 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 0.9754 mL 4.8772 mL 9.7545 mL
5 mM 0.1951 mL 0.9754 mL 1.9509 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 (protect from light, stored under nitrogen). 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 (protect from light, stored under nitrogen). 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 0.9754 mL 4.8772 mL 9.7545 mL 24.3862 mL
5 mM 0.1951 mL 0.9754 mL 1.9509 mL 4.8772 mL
10 mM 0.0975 mL 0.4877 mL 0.9754 mL 2.4386 mL
15 mM 0.0650 mL 0.3251 mL 0.6503 mL 1.6257 mL
20 mM 0.0488 mL 0.2439 mL 0.4877 mL 1.2193 mL
25 mM 0.0390 mL 0.1951 mL 0.3902 mL 0.9754 mL
30 mM 0.0325 mL 0.1626 mL 0.3251 mL 0.8129 mL
40 mM 0.0244 mL 0.1219 mL 0.2439 mL 0.6097 mL
50 mM 0.0195 mL 0.0975 mL 0.1951 mL 0.4877 mL
60 mM 0.0163 mL 0.0813 mL 0.1626 mL 0.4064 mL
80 mM 0.0122 mL 0.0610 mL 0.1219 mL 0.3048 mL
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PROTAC K-Ras Degrader-5 Related Classifications

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 K-Ras Degrader-53052745-16-8PROTACsRasCaspaseERKExtracellular signal regulated kinasesE3 ubiquitin ligase complexpancreatic cancer xenograftscancer cellscaspase 3/7proteasomal degradationKRas (G12D mutant)cereblonpERKcPARPubiquitinationInhibitorinhibitorinhibit

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