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MedKoo Cat#: 407153 | Name: Spautin-1
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Spautin-1 is a novel and potent autophagy inhibitor, which enhances imatinib-induced (MI) apoptosis in chronic myeloid leukemia. Autophagy has been proposed to play a role in MI resistance. Spautin-1 markedly inhibits IM-induced autophagy in CML cells by downregulating Beclin-1. Spautin-1 enhances IM-induced CML cell apoptosis by reducing the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2. Spautin-1 enhances IM-induced apoptosis by inactivating PI3K/AKT and activating downstream GSK3β, leading to downregulation of Mcl-1 and Bcl-2, which represents a promising approach to improve the efficacy of IM in the treatment of patients with CML.

Chemical Structure

Spautin-1
CAS#1262888-28-7

Theoretical Analysis

MedKoo Cat#: 407153

Name: Spautin-1

CAS#: 1262888-28-7

Chemical Formula: C15H11F2N3

Exact Mass: 271.0921

Molecular Weight: 271.27

Elemental Analysis: C, 66.42; H, 4.09; F, 14.01; N, 15.49

Price and Availability

Size Price Availability Quantity
5mg USD 270.00 2 Weeks
10mg USD 430.00 2 Weeks
50mg USD 730.00 2 Weeks
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Related CAS #
No Data
Synonym
Spautin-1; Spautin1; Spautin 1.
IUPAC/Chemical Name
6-Fluoro-N-[(4-Fluorophenyl)methyl]-4-quinazolinamine
InChi Key
AWIVHRPYFSSVOG-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H11F2N3/c16-11-3-1-10(2-4-11)8-18-15-13-7-12(17)5-6-14(13)19-9-20-15/h1-7,9H,8H2,(H,18,19,20)
SMILES Code
FC1=CC=C(CNC2=C3C=C(F)C=CC3=NC=N2)C=C1
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, 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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Spautin-1 inhibits ubiquitin-specific peptidases USP10 and USP13 with IC50s of 0.6-0.7 μM.
In vitro activity:
Spautin-1 may exhibit a promising approach to improving the efficacy of imatinib mesylate (IM) in the treatment of patients with chronic myeloid leukemia (CML). In CML cells, spautin-1 enhanced IM-induced apoptosis by inactivating PI3K/AKT and activating downstream GSK3β, leading to downregulation of Mcl-1 and Bcl-2. Reference: Int J Oncol. 2014 May;44(5):1661-8. https://pubmed.ncbi.nlm.nih.gov/24585095/
In vivo activity:
Spautin-1 treatment mitigated mild traumatic brain injury (TBI)-induced cognitive and memory dysfunction in mice, potentially through activation of caspase-3. After inducing TBIs in mice, spautin-1 administration significantly reversed aggravated neuronal injury, elevated activated microglia and CD86-occupied areas in TMEM119-positive cells, and suppressed θ, β, and γ oscillation power in the hippocampal CA1. Reference: Int Immunopharmacol. 2023 Apr;117:109906. https://pubmed.ncbi.nlm.nih.gov/36822083/
Solvent mg/mL mM comments
Solubility
DMSO 50.0 184.33
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 271.27 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.

Recalculate based on batch purity %
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:
1. Shao S, Li S, Qin Y, Wang X, Yang Y, Bai H, Zhou L, Zhao C, Wang C. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-8. doi: 10.3892/ijo.2014.2313. Epub 2014 Feb 27. PMID: 24585095; PMCID: PMC6904104. 2. Schott CR, Ludwig L, Mutsaers AJ, Foster RA, Wood GA. The autophagy inhibitor spautin-1, either alone or combined with doxorubicin, decreases cell survival and colony formation in canine appendicular osteosarcoma cells. PLoS One. 2018 Oct 29;13(10):e0206427. doi: 10.1371/journal.pone.0206427. PMID: 30372478; PMCID: PMC6205606. 3. Zhang LM, Zhang DX, Miao HT, Song RX, Shao JJ, Liu JZ, Jia SY, Xin Y, Wang H, Zhang W. Spautin-1 administration mitigates mild TBI-induced cognitive and memory dysfunction in mice via activation of caspase-3. Int Immunopharmacol. 2023 Apr;117:109906. doi: 10.1016/j.intimp.2023.109906. Epub 2023 Feb 21. PMID: 36822083. 4. Miao HT, Song RX, Xin Y, Wang LY, Lv JM, Liu NN, Wu ZY, Zhang W, Li Y, Zhang DX, Zhang LM. Spautin-1 Protects Against Mild TBI-Induced Anxiety-Like Behavior in Mice via Immunologically Silent Apoptosis. Neuromolecular Med. 2023 Sep;25(3):336-349. doi: 10.1007/s12017-023-08737-2. Epub 2023 Feb 6. PMID: 36745326.
In vitro protocol:
1. Shao S, Li S, Qin Y, Wang X, Yang Y, Bai H, Zhou L, Zhao C, Wang C. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-8. doi: 10.3892/ijo.2014.2313. Epub 2014 Feb 27. PMID: 24585095; PMCID: PMC6904104. 2. Schott CR, Ludwig L, Mutsaers AJ, Foster RA, Wood GA. The autophagy inhibitor spautin-1, either alone or combined with doxorubicin, decreases cell survival and colony formation in canine appendicular osteosarcoma cells. PLoS One. 2018 Oct 29;13(10):e0206427. doi: 10.1371/journal.pone.0206427. PMID: 30372478; PMCID: PMC6205606.
In vivo protocol:
1. Zhang LM, Zhang DX, Miao HT, Song RX, Shao JJ, Liu JZ, Jia SY, Xin Y, Wang H, Zhang W. Spautin-1 administration mitigates mild TBI-induced cognitive and memory dysfunction in mice via activation of caspase-3. Int Immunopharmacol. 2023 Apr;117:109906. doi: 10.1016/j.intimp.2023.109906. Epub 2023 Feb 21. PMID: 36822083. 2. Miao HT, Song RX, Xin Y, Wang LY, Lv JM, Liu NN, Wu ZY, Zhang W, Li Y, Zhang DX, Zhang LM. Spautin-1 Protects Against Mild TBI-Induced Anxiety-Like Behavior in Mice via Immunologically Silent Apoptosis. Neuromolecular Med. 2023 Sep;25(3):336-349. doi: 10.1007/s12017-023-08737-2. Epub 2023 Feb 6. PMID: 36745326.
1: Tong XP, Chen Y, Zhang SY, Xie T, Tian M, Guo MR, Kasimu R, Ouyang L, Wang JH. Key autophagic targets and relevant small-molecule compounds in cancer therapy. Cell Prolif. 2015 Feb;48(1):7-16. doi: 10.1111/cpr.12154. Epub 2014 Dec 4. Review. PubMed PMID: 25474301. 2: Chen S, Zhou L, Zhang Y, Leng Y, Pei XY, Lin H, Jones R, Orlowski RZ, Dai Y, Grant S. Targeting SQSTM1/p62 induces cargo loading failure and converts autophagy to apoptosis via NBK/Bik. Mol Cell Biol. 2014 Sep 15;34(18):3435-49. doi: 10.1128/MCB.01383-13. Epub 2014 Jul 7. PubMed PMID: 25002530; PubMed Central PMCID: PMC4135623. 3: Bouley SJ, Maginnis MS, Derdowski A, Gee GV, O'Hara BA, Nelson CD, Bara AM, Atwood WJ, Dugan AS. Host cell autophagy promotes BK virus infection. Virology. 2014 May;456-457:87-95. doi: 10.1016/j.virol.2014.03.009. Epub 2014 Apr 2. PubMed PMID: 24889228. 4: Shao S, Li S, Qin Y, Wang X, Yang Y, Bai H, Zhou L, Zhao C, Wang C. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-8. doi: 10.3892/ijo.2014.2313. Epub 2014 Feb 27. PubMed PMID: 24585095. 5: Correa RJ, Valdes YR, Peart TM, Fazio EN, Bertrand M, McGee J, Préfontaine M, Sugimoto A, DiMattia GE, Shepherd TG. Combination of AKT inhibition with autophagy blockade effectively reduces ascites-derived ovarian cancer cell viability. Carcinogenesis. 2014 Sep;35(9):1951-61. doi: 10.1093/carcin/bgu049. Epub 2014 Feb 22. PubMed PMID: 24562574; PubMed Central PMCID: PMC4146408. 6: Vakifahmetoglu-Norberg H, Yuan J. A degradative detour for mutant TP53. Autophagy. 2013 Dec;9(12):2158-60. doi: 10.4161/auto.26338. Epub 2013 Sep 30. PubMed PMID: 24145670. 7: Vakifahmetoglu-Norberg H, Kim M, Xia HG, Iwanicki MP, Ofengeim D, Coloff JL, Pan L, Ince TA, Kroemer G, Brugge JS, Yuan J. Chaperone-mediated autophagy degrades mutant p53. Genes Dev. 2013 Aug 1;27(15):1718-30. doi: 10.1101/gad.220897.113. Erratum in: Genes Dev. 2013 Sep 1;27(17):1947. PubMed PMID: 23913924; PubMed Central PMCID: PMC3744729. 8: Salabei JK, Cummins TD, Singh M, Jones SP, Bhatnagar A, Hill BG. PDGF-mediated autophagy regulates vascular smooth muscle cell phenotype and resistance to oxidative stress. Biochem J. 2013 May 1;451(3):375-88. doi: 10.1042/BJ20121344. PubMed PMID: 23421427; PubMed Central PMCID: PMC4040966. 9: Solano JD, González-Sánchez I, Cerbón MA, Guzmán Á, Martínez-Urbina MA, Vilchis-Reyes MA, Martínez-Zuñiga EC, Alvarado C, Quintero A, Díaz E. The products of the reaction between 6-amine-1,3-dimethyl uracil and bis-chalcones induce cytotoxicity with massive vacuolation in HeLa cervical cancer cell line. Eur J Med Chem. 2013 Feb;60:350-9. doi: 10.1016/j.ejmech.2012.12.021. Epub 2012 Dec 17. PubMed PMID: 23314048. 10: Mateo R, Nagamine CM, Spagnolo J, Méndez E, Rahe M, Gale M Jr, Yuan J, Kirkegaard K. Inhibition of cellular autophagy deranges dengue virion maturation. J Virol. 2013 Feb;87(3):1312-21. doi: 10.1128/JVI.02177-12. Epub 2012 Nov 21. PubMed PMID: 23175363; PubMed Central PMCID: PMC3554187. 11: Liu J, Xia H, Kim M, Xu L, Li Y, Zhang L, Cai Y, Norberg HV, Zhang T, Furuya T, Jin M, Zhu Z, Wang H, Yu J, Li Y, Hao Y, Choi A, Ke H, Ma D, Yuan J. Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13. Cell. 2011 Sep 30;147(1):223-34. doi: 10.1016/j.cell.2011.08.037. PubMed PMID: 21962518; PubMed Central PMCID: PMC3441147. (last updated: 4/20/2016).