1. Metabolic Enzyme/Protease
    Antibody-drug Conjugate/ADC Related
  2. Nampt
    Drug-Linker Conjugates for ADC

NAMPT inhibitor-linker 2 

Cat. No.: HY-112616
Handling Instructions

NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.

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

NAMPT inhibitor-linker 2 Chemical Structure

NAMPT inhibitor-linker 2 Chemical Structure

CAS No. : 2241014-82-2

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.

In Vitro

ADC-4 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively[1].
ADC-4 (0.01 nM-10 nM, 144 hours) inhibits cell proliferation of GIST-T1 cells, but does not affect the cell cycle[1].

Cell Proliferation Assay[1]

Cell Line: GIST-T1 cells
Concentration: 0.1 pM-10 nM
Incubation Time: 144 hours
Result: Inhibited the cell proliferation of GIST-T1 cells at 0.01-10 nM, and the inhibition remained unchanged after 1 nM.
In Vivo

ADC-4 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells[1].

Animal Model: Female scid-beige (SCID bg) mice[1]
Dosage: 20 mg/kg
Administration: A single intravenous injection (i.v.) for 28 days
Result: Significantly inhibited the growth of tumor in mice.
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6009 mL 8.0044 mL 16.0087 mL
5 mM 0.3202 mL 1.6009 mL 3.2017 mL
10 mM 0.1601 mL 0.8004 mL 1.6009 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

624.66

Formula

C₃₄H₃₃FN₆O₅

CAS No.

2241014-82-2

SMILES

FC1=CC(NC([[email protected]@H]2[[email protected]](C2)C3=CN=CC=C3)=O)=CC=C1CNC(C4=CC=C(N5CCN(C(CCN6C(C=CC6=O)=O)=O)CC5)C=C4)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
NAMPT inhibitor-linker 2
Cat. No.:
HY-112616
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NAMPT inhibitor-linker 2

Cat. No.: HY-112616