Fmoc-Val-Cit-PAB-PNP

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
500mg	$550	Check With Us
1g	$850	Check With Us
5g	$2150	Check With Us

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Cat #: V21222 CAS #: 863971-53-3 Purity ≥ 98%

Description: Fmoc-Val-Cit-PAB-PNP is a linker for Antibody-Drug-Conjugation (ADC). The Val-Cit will specifically be cleaved by catepsin B. Because this enzyme is only present in the lysosome, the ADC payload will only be released in the cell. The azido group will react with DBCO, BCN or other alkyne groups through click chemistry. The hydrophilic PEG spacer increases solubility in aqueous media.

References: [1]. Dubowchik GM, et al. Cathepsin B-labile dipeptide linkers for lysosomal release of doxorubicin from internalizing immunoconjugates: model studies of enzymatic drug release and antigen-specific in vitro anticancer activity. Bioconjug Chem. 2002 Jul-Aug;13(4):855-69.

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Physicochemical and Storage Information
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Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	766.80
Molecular Formula	C40H42N6O10
CAS No.	863971-53-3
SMILES Code	O=C(OCC1=CC=C(NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)NC(OCC2C(C=CC=C3)=C3C4=C2C=CC=C4)=O)=O)=O)C=C1)OC5=CC=C([N+]([O-])=O)C=C5
Synonyms	Fmoc-Val-Cit-PAB-PNP;

Protocol	In Vitro	Fmoc-Val-Cit-PAB-PNP contains peptide sequence degradable by a lysosome enzyme. 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.
Protocol	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. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.3041 mL	6.5206 mL	13.0412 mL	26.0824 mL
5mM	0.2608 mL	1.3041 mL	2.6082 mL	5.2165 mL
10mM	0.1304 mL	0.6521 mL	1.3041 mL	2.6082 mL
20mM	0.0652 mL	0.3260 mL	0.6521 mL	1.3041 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.