2. PROTAC Immunology/Inflammation
  3. PROTACs PD-1/PD-L1
  4. PROTAC PD-L1 degrader-1

PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745)).

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

PROTAC PD-L1 degrader-1 Chemical Structure

PROTAC PD-L1 degrader-1 Chemical Structure

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PROTAC PD-L1 degrader-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745))[1].

IC50 & Target[1]

Cereblon

131.77 μM (Kd)

In Vitro

PROTAC PD-L1 degrader-1 (compound PA8; 0.078-10 μM; 24 h) displays a significant degradation effect on PD-L1 protein in 4T1 cells across in a dose-dependent manner[1].
PROTAC PD-L1 degrader-18 binds specifically to CRBN and PD-L1 with Kd values of 131.77 μM and 59.2 μM, respectively, and both are concentration dependent[1].

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

PROTAC PD-L1 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: 4T1 cells
Concentration: 0.078 μM, 0.156 μM, 0.312 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Displayed a significant degradation effect on PD-L1 protein in 4T1 cells.
In Vivo

PROTAC PD-L1 degrader-18 (30-60 mg/kg; ip; once daily for 15 days) inhibits tumor volume and tumor weight in 4T1 bearing mice models[1].
Pharmacokinetic Parameters of PROTAC PD-L1 degrader-1 (compound PA8) in Male Sprague-Dawley rats[1].
1.19

Plasma PK properties CL (mL/min/kg) Vss (L/kg) (ng▪h/mL) Tmax (h) Cmax (ng/mL) T1/2 (h)
i.v (3 mg/kg) 471.0 23.0 / / 0.952
i.p (30 mg/kg) / / 2.0 217.0 5.3

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

Animal Model: 6-8 week old female BALB/c mice injected with 4T1 cells[1].
Dosage: 30 and 60 mg/kg
Administration: ip; once daily for 15 days
Result: The antitumor effect can be obviously observed.
Molecular Weight

777.95

Formula

C45H55N5O7
SMILES

O=C(NCCNCC1=CC=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)N=C1OC)CCCCCCCCNC(COC4=CC=C(C(CC5)C(NC5=O)=O)C=C4)=O
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 PD-L1 degrader-1 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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 PD-L1 degrader-1PROTACsPD-1/PD-L1PD-1/Programmed death-ligand 1PD-L1-PROTAC degraderCRBNbreast cancerInhibitorinhibitorinhibit

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PROTAC PD-L1 degrader-1
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