WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H525896
CAS#: 1644443-47-9
Description: Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34.
Hodoodo Cat#: H525896
Name: Autophinib
CAS#: 1644443-47-9
Chemical Formula: C14H11ClN6O3
Exact Mass: 346.06
Molecular Weight: 346.731
Elemental Analysis: C, 48.50; H, 3.20; Cl, 10.22; N, 24.24; O, 13.84
Synonym: Autophinib
IUPAC/Chemical Name: 6-Chloro-N-(5-methyl-1H-pyrazol-3-yl)-2-(4-nitrophenoxy)pyrimidin-4-amine
InChi Key: CEUMAXLRGBKFQP-UHFFFAOYSA-N
InChi Code: InChI=1S/C14H11ClN6O3/c1-8-6-13(20-19-8)17-12-7-11(15)16-14(18-12)24-10-4-2-9(3-5-10)21(22)23/h2-7H,1H3,(H2,16,17,18,19,20)
SMILES Code: O=[N+](C1=CC=C(OC2=NC(Cl)=CC(NC3=NNC(C)=C3)=N2)C=C1)[O-]
Appearance: Solid powder
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
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
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 14.0 | 40.32 |
The following data is based on the product molecular weight 346.73 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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Yang Y, Chen D, Liu H, Yang K. Increased expression of lncRNA CASC9 promotes tumor progression by suppressing autophagy-mediated cell apoptosis via the AKT/mTOR pathway in oral squamous cell carcinoma. Cell Death Dis. 2019 Jan 17;10(2):41. doi: 10.1038/s41419-018-1280-8. PMID: 30674868; PMCID: PMC6381212.
2: Robke L, Laraia L, Carnero Corrales MA, Konstantinidis G, Muroi M, Richters A, Winzker M, Engbring T, Tomassi S, Watanabe N, Osada H, Rauh D, Waldmann H, Wu YW, Engel J. Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34. Angew Chem Int Ed Engl. 2017 Jul 3;56(28):8153-8157. doi: 10.1002/anie.201703738. Epub 2017 Jun 12. PMID: 28544137.
3: Li H, Li M, Chen K, Li Y, Yang Z, Zhou Z. The circadian clock gene ARNTL overexpression suppresses oral cancer progression by inducing apoptosis via activating autophagy. Med Oncol. 2022 Sep 30;39(12):244. doi: 10.1007/s12032-022-01832-7. PMID: 36180647.
4: Duan J, Chen H, Xu D, Li Y, Li X, Cheng J, Hua R, Zhang Z, Yang L, Li Q. 17β-estradiol improves the developmental ability, inhibits reactive oxygen species levels and apoptosis of porcine oocytes by regulating autophagy events. J Steroid Biochem Mol Biol. 2021 May;209:105826. doi: 10.1016/j.jsbmb.2021.105826. Epub 2021 Feb 10. PMID: 33581253.
5: Aleksandrova KV, Suvorova II. Evaluation of the Effectiveness of Various Autophagy Inhibitors in A549 Cancer Stem Cells. Acta Naturae. 2023 Jan- Mar;15(1):19-25. doi: 10.32607/actanaturae.11891. PMID: 37153502; PMCID: PMC10154774.
6: Li Y, Li J, Wei SS, Du J. Lipopolysaccharide-induced Trigeminal Ganglion Nerve Fiber Damage is Associated with Autophagy Inhibition. Curr Med Sci. 2023 Jun;43(3):489-495. doi: 10.1007/s11596-023-2739-0. Epub 2023 Jun 6. PMID: 37278832.
7: Duan J, Chen H, Li Y, Xu D, Li X, Zhang Z, Cheng J, Yang L, Li Q. 17β-Estradiol Enhances Porcine Meiosis Resumption from Autophagy-Induced Gap Junction Intercellular Communications and Connexin 43 Phosphorylation via the MEK/ERK Signaling Pathway. J Agric Food Chem. 2021 Oct 13;69(40):11847-11855. doi: 10.1021/acs.jafc.1c04212. Epub 2021 Oct 5. PMID: 34609142.
8: Hanelova K, Raudenska M, Kratochvilova M, Navratil J, Vicar T, Bugajova M, Gumulec J, Masarik M, Balvan J. Autophagy modulators influence the content of important signalling molecules in PS-positive extracellular vesicles. Cell Commun Signal. 2023 May 24;21(1):120. doi: 10.1186/s12964-023-01126-z. PMID: 37226246; PMCID: PMC10210466.
9: Relic B, Deroyer C, Malaise O, Plener Z, Gillet P, de Seny D, Malaise MG. TFEB phosphorylation on Serine 211 is induced by autophagy in human synovial fibroblasts and by p62/SQSTM1 overexpression in HEK293 cells. Biochem J. 2021 Aug 27;478(16):3145-3155. doi: 10.1042/BCJ20210174. PMID: 34405859; PMCID: PMC8421036.
10: Liu H, Gong X, Yang K. Overexpression of the clock gene Per2 suppresses oral squamous cell carcinoma progression by activating autophagy via the PI3K/AKT/mTOR pathway. J Cancer. 2020 Mar 26;11(12):3655-3666. doi: 10.7150/jca.42771. PMID: 32284762; PMCID: PMC7150464.
11: Yang G, Yang Y, Tang H, Yang K. Loss of the clock gene Per1 promotes oral squamous cell carcinoma progression via the AKT/mTOR pathway. Cancer Sci. 2020 May;111(5):1542-1554. doi: 10.1111/cas.14362. Epub 2020 Mar 18. PMID: 32086839; PMCID: PMC7226219.