Synonym
ASP4132; ASP-4132; ASP 4132
IUPAC/Chemical Name
[6-[1-[(6-Methoxy-3-pyridinyl)methyl]-4-piperidinyl]-1H-benzimidazol-2-yl][4-[[4-(trifluoromethyl)phenyl]methyl]-1-piperazinyl]methanone
InChi Key
KKRRTZFDLYCBDK-UHFFFAOYSA-N
InChi Code
InChI=1S/C32H35F3N6O2/c1-43-29-9-4-23(19-36-29)21-39-12-10-24(11-13-39)25-5-8-27-28(18-25)38-30(37-27)31(42)41-16-14-40(15-17-41)20-22-2-6-26(7-3-22)32(33,34)35/h2-9,18-19,24H,10-17,20-21H2,1H3,(H,37,38)
SMILES Code
O=C(C1=NC2=CC=C(C3CCN(CC4=CC=C(OC)N=C4)CC3)C=C2N1)N5CCN(CC6=CC=C(C(F)(F)F)C=C6)CC5
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
592.67
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Xia YC, Zha JH, Sang YH, Yin H, Xu GQ, Zhen J, Zhang Y, Yu BT. AMPK
activation by ASP4132 inhibits non-small cell lung cancer cell growth. Cell
Death Dis. 2021 Apr 6;12(4):365. doi: 10.1038/s41419-021-03655-2. PMID:
33824293; PMCID: PMC8024326.
2: Janku F, LoRusso P, Mansfield AS, Nanda R, Spira A, Wang T, Melhem-Bertrandt
A, Sugg J, Ball HA. First-in-human evaluation of the novel mitochondrial complex
I inhibitor ASP4132 for treatment of cancer. Invest New Drugs. 2021
Oct;39(5):1348-1356. doi: 10.1007/s10637-021-01112-7. Epub 2021 Apr 8. PMID:
33830407.
3: Kuramoto K, Yamada H, Shin T, Sawada Y, Azami H, Yamada T, Nagashima T,
Ohnuki K. Development of a potent and orally active activator of adenosine
monophosphate-activated protein kinase (AMPK), ASP4132, as a clinical candidate
for the treatment of human cancer. Bioorg Med Chem. 2020 Mar 1;28(5):115307.
doi: 10.1016/j.bmc.2020.115307. Epub 2020 Jan 8. PMID: 32007387.
4: Kuramoto K, Sawada Y, Yamada T, Nagashima T, Ohnuki K, Shin T. Novel Indirect
AMP-Activated Protein Kinase Activators: Identification of a Second-Generation
Clinical Candidate with Improved Physicochemical Properties and Reduced hERG
Inhibitory Activity. Chem Pharm Bull (Tokyo). 2020;68(5):452-465. doi:
10.1248/cpb.c20-00015. PMID: 32378543.
