2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs c-Met/HGFR
  4. PROTAC c-Met degrader-1

PROTAC c-Met degrader-1 is a selective and orally active c-Met PROTAC degrader with a DC50 of 6.21 nM against c-Met. PROTAC c-Met degrader-1 induces CRBN-dependent ubiquitination and proteasomal degradation of c-Met. PROTAC c-Met degrader-1 induces G0/G1 phase arrest in c-Met-dependent cancer cells. PROTAC c-Met degrader-1 kills c-Met-dependent cancer cells. PROTAC c-Met degrader-1 inhibits tumor growth in animal models. PROTAC c-Met degrader-1 can be used for the research of gastric cancer.
(Pink: c-Met ligand (HY-13404); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W074901)).

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

PROTAC c-Met degrader-1

PROTAC c-Met degrader-1 Chemical Structure

CAS No. : 3056647-52-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

PROTAC c-Met degrader-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

PROTAC c-Met degrader-1 is a selective and orally active c-Met PROTAC degrader with a DC50 of 6.21 nM against c-Met. PROTAC c-Met degrader-1 induces CRBN-dependent ubiquitination and proteasomal degradation of c-Met. PROTAC c-Met degrader-1 induces G0/G1 phase arrest in c-Met-dependent cancer cells. PROTAC c-Met degrader-1 kills c-Met-dependent cancer cells. PROTAC c-Met degrader-1 inhibits tumor growth in animal models. PROTAC c-Met degrader-1 can be used for the research of gastric cancer[1]. (Pink: c-Met ligand (HY-13404); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W074901)).

IC50 & Target

c-Met

6.21 nM (DC50)

In Vitro

PROTAC c-Met degrader-1 (Met-DD4) (0.1954-200 nM; 1-24 h) potently and dose-dependently degrades c-Met in MKN-45 cells with a DC50 of 6.21 nM, achieving 96.83% maximal degradation and time-dependent degradation that peaks at 16 h[1].
PROTAC c-Met degrader-1 (72 h) potently inhibits the proliferation of c-Met-addicted MKN-45 cells with an IC50 of 4.37 nM[1].
PROTAC c-Met degrader-1 induces robust c-Met degradation and blocks c-Met-Akt signaling in Hs746T and PC-9 cells[1].
PROTAC c-Met degrader-1 (100 nM; 1-24 h) induces c-Met degradation in MKN-45 cells via a CRBN-mediated ubiquitin-proteasome pathway[1].
PROTAC c-Met degrader-1 (100 nM; 24 h) exhibits high degradation selectivity for c-Met in MKN-45 cells, with no other proteins significantly downregulated more than 4-fold[1].

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

PROTAC c-Met degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MKN-45
Concentration: 100 nM
Incubation Time: 1 h, 2 h, 3 h, 4 h, 8 h,16 h, 24 h
Result: Had c-Met degradation significantly reversed by pretreatment with 5 μM capmatinib, 10 μM pomalidomide, 5 μM MG132, or 5 μM MLN4924.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-∞ MRT0-∞
Rat[1] 10 mg/kg p.o. 4.13 h 2.00 h 70.7 ng/mL 411 ng·h/mL 6.66 h
Rat[1] 10 mg/kg i.v. 5.35 h 0.08 h 1650 ng/mL 2518 ng·h/mL 2.56 h
In Vivo

PROTAC c-Met degrader-1 (Met-DD4) (10-40 mg/kg; p.o.; daily; 21 days) dose-dependently retards MKN-45 xenograft tumor growth in nude mice, induces robust c-Met degradation in tumor tissues, and maintains a favorable safety profile over 21 days of daily oral administration[1].

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

Animal Model: BALB/c nude (female) injected with MKN-45 cells[1]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: p.o.; daily; 21 days
Result: Exhibited dose-dependent tumor growth retardation.
Induced degradation of total and phosphorylated c-Met in tumor tissues compared to vehicle control at all three doses.
Caused no significant body weight loss in any treated group.
Showed normal organ morphology in lung, liver, spleen, kidney, and heart with no evidence of systemic toxicity.
Molecular Weight

820.87

Formula

C45H41FN10O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC1=C(C=CC(C(C=N2)=NN3C2=NC=C3CC4=CC5=C(C=C4)N=CC=C5)=C1)C(N6CCC(CN7CCN(C8=CC9=C(C=C8)C(N(C9=O)C(C(N%10)=O)CCC%10=O)=O)CC7)CC6)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (121.82 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2182 mL 6.0911 mL 12.1822 mL
5 mM 0.2436 mL 1.2182 mL 2.4364 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. 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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. 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 1.2182 mL 6.0911 mL 12.1822 mL 30.4555 mL
5 mM 0.2436 mL 1.2182 mL 2.4364 mL 6.0911 mL
10 mM 0.1218 mL 0.6091 mL 1.2182 mL 3.0455 mL
15 mM 0.0812 mL 0.4061 mL 0.8121 mL 2.0304 mL
20 mM 0.0609 mL 0.3046 mL 0.6091 mL 1.5228 mL
25 mM 0.0487 mL 0.2436 mL 0.4873 mL 1.2182 mL
30 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
40 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7614 mL
50 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6091 mL
60 mM 0.0203 mL 0.1015 mL 0.2030 mL 0.5076 mL
80 mM 0.0152 mL 0.0761 mL 0.1523 mL 0.3807 mL
100 mM 0.0122 mL 0.0609 mL 0.1218 mL 0.3046 mL
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PROTAC c-Met degrader-1 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 c-Met degrader-13056647-52-7PROTACsc-Met/HGFRc-Met-addicted cancer cellsnude micePC-9 cellsubiquitinationG0/G1 phase arrestCRBNMKN-45 cellsproteasomal degradationHs746T cellsc-MetInhibitorinhibitorinhibit

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