1. Metabolic Enzyme/Protease
  2. NAMPT
  3. A-1293201

A-1293201 is a substrate-independent NAMPT inhibitor with antitumor activity. A-1293201 effectively reduces the total cellular NAD+/NADH (NADt) level, subsequently leading to ATP depletion and cancer cell death. In addition, A-1293201 can effectively overcome the acquired resistance mechanism of the NAMPT Y18 mutant to CHS-828 (HY-10079).

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A-1293201 Chemical Structure

A-1293201 Chemical Structure

CAS No. : 1375557-33-7

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Description

A-1293201 is a substrate-independent NAMPT inhibitor with antitumor activity. A-1293201 effectively reduces the total cellular NAD+/NADH (NADt) level, subsequently leading to ATP depletion and cancer cell death. In addition, A-1293201 can effectively overcome the acquired resistance mechanism of the NAMPT Y18 mutant to CHS-828 (HY-10079)[1].

Cellular Effect
Cell Line Type Value Description References
PC-3 IC50
56 nM
Compound: 58
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay
[PMID: 28610984]
Molecular Weight

365.43

Formula

C21H23N3O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CC2=C(C=CC=C2)C1)NC3=CC=C(C(NC[C@H]4COCC4)=O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (171.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7365 mL 13.6825 mL 27.3650 mL
5 mM 0.5473 mL 2.7365 mL 5.4730 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7365 mL 13.6825 mL 27.3650 mL 68.4126 mL
5 mM 0.5473 mL 2.7365 mL 5.4730 mL 13.6825 mL
10 mM 0.2737 mL 1.3683 mL 2.7365 mL 6.8413 mL
15 mM 0.1824 mL 0.9122 mL 1.8243 mL 4.5608 mL
20 mM 0.1368 mL 0.6841 mL 1.3683 mL 3.4206 mL
25 mM 0.1095 mL 0.5473 mL 1.0946 mL 2.7365 mL
30 mM 0.0912 mL 0.4561 mL 0.9122 mL 2.2804 mL
40 mM 0.0684 mL 0.3421 mL 0.6841 mL 1.7103 mL
50 mM 0.0547 mL 0.2737 mL 0.5473 mL 1.3683 mL
60 mM 0.0456 mL 0.2280 mL 0.4561 mL 1.1402 mL
80 mM 0.0342 mL 0.1710 mL 0.3421 mL 0.8552 mL
100 mM 0.0274 mL 0.1368 mL 0.2737 mL 0.6841 mL
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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:
A-1293201
Cat. No.:
HY-125147
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