Spautin-1
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MedKoo CAT#: 407153

CAS#: 1262888-28-7

Description: 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

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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

Size Price Shipping out time Quantity
25mg USD 220 2 Weeks
50mg USD 350 2 Weeks
100mg USD 650 2 Weeks
200mg USD 1050 2 Weeks
500mg USD 1750 2 Weeks
1g USD 2450 2 Weeks
2g USD 3650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-09. Prices are subject to change without notice.

Spautin-1, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).

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

Handling Instructions:

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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).