1. Antibody-drug Conjugate/ADC Related
  2. ADC Linker
  3. Fmoc-Val-Cit-PAB-PNP

Fmoc-Val-Cit-PAB-PNP 

Cat. No.: HY-41189 Purity: ≥98.0%
COA Handling Instructions

Fmoc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Val-Cit-PAB-PNP has superior plasma stability comparable to that of non-cleavable linkers.

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

Fmoc-Val-Cit-PAB-PNP Chemical Structure

Fmoc-Val-Cit-PAB-PNP Chemical Structure

CAS No. : 863971-53-3

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Estimated Time of Arrival: December 31
100 mg USD 190 In-stock
Estimated Time of Arrival: December 31
250 mg USD 320 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Fmoc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Val-Cit-PAB-PNP has superior plasma stability comparable to that of non-cleavable linkers[1][2][3].

IC50 & Target

Protease Cleavable

 

Cleavable

 

In Vitro

Fmoc-Val-Cit-PAB-PNP contains peptide sequence degradable by a lysosome enzyme[1].
Cathepsin B in the lysosome cleaves the peptide bond between Cit-PAB of dipeptide linkers containing Valine (Val)-citrulline (Cit) and p-aminobenzylalcohol (PAB). When PAB and a drug are binded covalently with carbamate bonds, the drug can be released by hydrolysis after cleavage of the peptide bond between Cit-PAB. Antibody-drug conjugates (ADCs) has been developed using this mechanism[2].

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

In Vivo

Fmoc-Val-Cit-PAB-PNP linker stabilization in the mouse is an essential prerequisite for designing successful efficacy and safety studies in rodents during preclinical stages of ADC programs[3].
Conjugation site plays an important role in determining VC-PABC linker stability in mouse plasma, and that the stability of the linker positively correlates with ADC cytotoxic potency both in vitro and in vivo[3].

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

Molecular Weight

766.80

Appearance

Solid

Formula

C40H42N6O10

CAS No.
Sequence Shortening

Fmoc-V-Cit-PAB-PNP

SMILES

CC(C)[[email protected]@H](C(N[[email protected]@H](CCCNC(N)=O)C(NC1=CC=C(COC(OC2=CC=C([N+]([O-])=O)C=C2)=O)C=C1)=O)=O)NC(OCC3C4=C(C5=C3C=CC=C5)C=CC=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (52.16 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3041 mL 6.5206 mL 13.0412 mL
5 mM 0.2608 mL 1.3041 mL 2.6082 mL
10 mM 0.1304 mL 0.6521 mL 1.3041 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5.25 mg/mL (6.85 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: ≥98.0%

References
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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.

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Product Name:
Fmoc-Val-Cit-PAB-PNP
Cat. No.:
HY-41189
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