GLPBio

Nitro-PDS-Tubulysin M

Catalog No.: GC36748Purity:>98%
COASDSData Sheet
Nitro-PDS-Tubulysin M is a drug-linker conjugate for ADC with potent antitumor activity by using Tubulysin M (a tubulin polymerization inhibitor), linked via the ADC linker Nitro-PDS.

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Nitro-PDS-Tubulysin M
Cas No.: 1941168-69-9
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Description

Nitro-PDS-Tubulysin M has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. Nitro-PDS-Tubulysin M is used for the antibody-drug conjugates (ADC) to treat various diseases or disorders, e.g. characterized by the overexpression of a tumor antigen[1,2].

ADC2-2 (anti-CD22 10F4v3 LC K149C Nitro-PDS-Tubulysin M) displays target-specific killing in WSU-DLCL2 human diffuse large B-cell lymphoma tumors with IC50 of 0.147 nM, and ADC2-1 (anti-Napi2b 10H1.11.4B LC K149C Nitro-PDS-Tubulysin M) displays target-specific killing in human ovarian cancer IGROV-1 and OVCAR-3x2.1 with IC50s of 2.07 nM, 1.004 nM, respectively[1].

[1]. FLYGARE, John A, et al. Quaternary amine compounds and antibody-drug conjugates thereof. WO2016090050A1. [2]. Staben LR, et al. Targeted drug delivery through the traceless release of tertiary and heteroaryl amines from antibody-drug conjugates. Nat Chem. 2016 Dec;8(12):1112-1119.

Chemical Properties

CAS No.
1941168-69-9
SMILES
O=C(O)[C@@H](C)C[C@@H](NC(C1=CSC([C@H](OC(C)=O)C[C@@H](N(C)C([C@@H](NC([C@@H]2[N+](CC3=CC=C(NC(OC[C@H](SSC4=CC=C([N+]([O-])=O)N=C4)C)=O)C=C3)(C)CCCC2)=O)[C@@H](C)CC)=O)C(C)C)=N1)=O)CC5=CC=CC=C5
Molecular Formula
C54H73N8O11S3
Molecular Weight
1106.4
Solubility
Soluble in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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