Y15 hydrochloride
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MedKoo CAT#: 407352

CAS#: 4506-66-5 (HCl)

Description: Y15 hydrochloride, also known as FAK Inhibitor 14, is a direct FAK autophosphorylation inhibitor, blocking phosphorylation of Y397 with an IC50 value of about 1 μM. Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Y15 was shown to decrease cancer growth in vitro and in vivo.


Chemical Structure

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Y15 hydrochloride
CAS# 4506-66-5 (HCl)

Theoretical Analysis

MedKoo Cat#: 407352
Name: Y15 hydrochloride
CAS#: 4506-66-5 (HCl)
Chemical Formula: C6H14Cl4N4
Exact Mass:
Molecular Weight: 284.006
Elemental Analysis: C, 25.37; H, 4.97; Cl, 49.93; N, 19.73

Price and Availability

Size Price Availability Quantity
1.0g USD 150.0 Ready to ship
2.0g USD 250.0 Ready to ship
5.0g USD 550.0 Ready to ship
10.0g USD 950.0 Ready to ship
20.0g USD 1750.0 Ready to ship
50.0g USD 3250.0 2 Weeks
Bulk inquiry

Synonym: Y15 hydrochloride; Y15 tetrahydrochloride; Y 15; Y-15. FAK Inhibitor 14.

IUPAC/Chemical Name: 1,2,4,5-benzenetetramine tetrahydrochloride

InChi Key: BZDGCIJWPWHAOF-UHFFFAOYSA-N

InChi Code: InChI=1S/C6H10N4.4ClH/c7-3-1-4(8)6(10)2-5(3)9;;;;/h1-2H,7-10H2;4*1H

SMILES Code: NC1=CC(N)=C(N)C=C1N.[H]Cl.[H]Cl.[H]Cl.[H]Cl

Appearance: Light green to green 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: 292159

Biological target: Y15 is an inhibitor of focal adhesion kinase (FAK).
In vitro activity: In each cell line Y15 inhibited pY397 and total FAK expression in a dose-dependent manner. TT was the most sensitive cell line with effective inhibition of pY397 expression by 3 μM Y15 (Figure 2A). TPC1 cells had inhibition of phosphorylated FAK and total FAK expression at 30 μM Y15 (Figure 2B). K1 had Y397-FAK and FAK inhibition at 50 μM (Figure 2C) and BCPAP had inhibition of pY397 and FAK expression levels at 40 μM Y15 (Figure 2D). Thus, Y15 decreased pY397 and total FAK levels in a dose-dependent manner, most in the medullary thyroid cancer cell line and to a lesser extent in the papillary thyroid cancer cell lines. Reference: Oncotarget. 2014 Sep; 5(17): 7945–7959. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4202172/
In vivo activity: Although weight-loss was similar in both infected groups [Fig. 2B], three doses of Y15 were sufficient to significantly extend survival time by 3 days and increase survival [Fig. 2C]. Importantly, DMSO-treated mice either succumbed to the infection (4/8) or were euthanized based on reaching symptom end-points before reaching body weight-loss cut-off. In contrast, most (7/8) Y15-treated mice were euthanized due to reaching body weight-loss cut-off with mild symptoms being observed. These data indicate that short-term prophylactic intranasal administration of Y15 results in prolonged survival of an extremely susceptible host. Reference: Virology. 2019 Aug;534:54-63. https://pubmed.ncbi.nlm.nih.gov/31176924/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.1 70.77
Water 28.05 98.77

Preparing Stock Solutions

The following data is based on the product molecular weight 284.006 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. O'Brien S, Golubovskaya VM, Conroy J, Liu S, Wang D, Liu B, Cance WG. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 Sep 15;5(17):7945-59. doi: 10.18632/oncotarget.2381. PMID: 25277206; PMCID: PMC4202172. 2. Huang G, Ho B, Conroy J, Liu S, Qiang H, Golubovskaya V. The microarray gene profiling analysis of glioblastoma cancer cells reveals genes affected by FAK inhibitor Y15 and combination of Y15 and temozolomide. Anticancer Agents Med Chem. 2014 Jan;14(1):9-17. doi: 10.2174/18715206113139990141. PMID: 23387973; PMCID: PMC3883957. 3. Bergmann S, Elbahesh H. Targeting the proviral host kinase, FAK, limits influenza a virus pathogenesis and NFkB-regulated pro-inflammatory responses. Virology. 2019 Aug;534:54-63. doi: 10.1016/j.virol.2019.05.020. Epub 2019 Jun 1. PMID: 31176924. 4. Zhang H, Shao H, Golubovskaya VM, Chen H, Cance W, Adjei AA, Dy GK. Efficacy of focal adhesion kinase inhibition in non-small cell lung cancer with oncogenically activated MAPK pathways. Br J Cancer. 2016 Jul 12;115(2):203-11. doi: 10.1038/bjc.2016.190. Epub 2016 Jun 23. PMID: 27336608; PMCID: PMC4947704.
In vitro protocol: 1. O'Brien S, Golubovskaya VM, Conroy J, Liu S, Wang D, Liu B, Cance WG. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 Sep 15;5(17):7945-59. doi: 10.18632/oncotarget.2381. PMID: 25277206; PMCID: PMC4202172. 2. Huang G, Ho B, Conroy J, Liu S, Qiang H, Golubovskaya V. The microarray gene profiling analysis of glioblastoma cancer cells reveals genes affected by FAK inhibitor Y15 and combination of Y15 and temozolomide. Anticancer Agents Med Chem. 2014 Jan;14(1):9-17. doi: 10.2174/18715206113139990141. PMID: 23387973; PMCID: PMC3883957.
In vivo protocol: 1. Bergmann S, Elbahesh H. Targeting the proviral host kinase, FAK, limits influenza a virus pathogenesis and NFkB-regulated pro-inflammatory responses. Virology. 2019 Aug;534:54-63. doi: 10.1016/j.virol.2019.05.020. Epub 2019 Jun 1. PMID: 31176924. 2. Zhang H, Shao H, Golubovskaya VM, Chen H, Cance W, Adjei AA, Dy GK. Efficacy of focal adhesion kinase inhibition in non-small cell lung cancer with oncogenically activated MAPK pathways. Br J Cancer. 2016 Jul 12;115(2):203-11. doi: 10.1038/bjc.2016.190. Epub 2016 Jun 23. PMID: 27336608; PMCID: PMC4947704.

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1: Golubovskaya V, O'Brien S, Ho B, Heffler M, Conroy J, Hu Q, Wang D, Liu S, Cance WG. Down-regulation of ALDH1A3, CD44 or MDR1 sensitizes resistant cancer cells to FAK autophosphorylation inhibitor Y15. J Cancer Res Clin Oncol. 2015 Sep;141(9):1613-31. doi: 10.1007/s00432-015-1924-3. PubMed PMID: 25656374.

2: Golubovskaya V, Curtin L, Groman A, Sexton S, Cance WG. In vivo toxicity, metabolism and pharmacokinetic properties of FAK inhibitor 14 or Y15 (1, 2, 4, 5-benzenetetramine tetrahydrochloride). Arch Toxicol. 2015 Jul;89(7):1095-101. doi: 10.1007/s00204-014-1290-y. PubMed PMID: 24915938.

3: O'Brien S, Golubovskaya VM, Conroy J, Liu S, Wang D, Liu B, Cance WG. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 Sep 15;5(17):7945-59. PubMed PMID: 25277206; PubMed Central PMCID: PMC4202172.

4: O'Brien S, Golubovskaya VM, Conroy J, Liu S, Wang D, Liu B, Cance WG. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 Aug 25. [Epub ahead of print] PubMed PMID: 25210005.

5: Huang G, Ho B, Conroy J, Liu S, Qiang H, Golubovskaya V. The microarray gene profiling analysis of glioblastoma cancer cells reveals genes affected by FAK inhibitor Y15 and combination of Y15 and temozolomide. Anticancer Agents Med Chem. 2014 Jan;14(1):9-17. PubMed PMID: 23387973; PubMed Central PMCID: PMC3883957.

6: Qiao F, Gao CY, Tripathi BK, Zelenka PS. Distinct functions of Cdk5(Y15) phosphorylation and Cdk5 activity in stress fiber formation and organization. Exp Cell Res. 2008 Nov 15;314(19):3542-50. doi: 10.1016/j.yexcr.2008.08.023. PubMed PMID: 18838073.

7: Chang TS, Lee KS, Lee GY, Jeon SD, So DS, Khil LY, Chung MK, Moon CK. NQ-Y15 inhibits the calcium mobilization by elevation of cyclic AMP in rat platelets. Biol Pharm Bull. 2001 May;24(5):480-3. PubMed PMID: 11379764.

8: Zhang H, Shao H, Golubovskaya VM, Chen H, Cance W, Adjei AA, Dy GK. Efficacy of focal adhesion kinase inhibition in non-small cell lung cancer with oncogenically activated MAPK pathways. Br J Cancer. 2016 Jul 12;115(2):203-11. doi: 10.1038/bjc.2016.190. PubMed PMID: 27336608; PubMed Central PMCID: PMC4947704.

9: Heffler M, Golubovskaya VM, Dunn KM, Cance W. Focal adhesion kinase autophosphorylation inhibition decreases colon cancer cell growth and enhances the efficacy of chemotherapy. Cancer Biol Ther. 2013 Aug;14(8):761-72. doi: 10.4161/cbt.25185. PubMed PMID: 23792569; PubMed Central PMCID: PMC3841216.

10: Goulston LM, Kiran A, Javaid MK, Soni A, White KM, Hart DJ, Spector TD, Arden NK. Does obesity predict knee pain over fourteen years in women, independently of radiographic changes? Arthritis Care Res (Hoboken). 2011 Oct;63(10):1398-406. doi: 10.1002/acr.20546. PubMed PMID: 21739621.

11: Chang TS, Kim HM, Lee KS, Khil LY, Mar WC, Ryu CK, Moon CK. Thromboxane A2 synthase inhibition and thromboxane A2 receptor blockade by 2-[(4-cyanophenyl)amino]-3-chloro-1,4-naphthalenedione (NQ-Y15) in rat platelets. Biochem Pharmacol. 1997 Jul 15;54(2):259-68. PubMed PMID: 9271330.

12: Golubovskaya VM, Huang G, Ho B, Yemma M, Morrison CD, Lee J, Eliceiri BP, Cance WG. Pharmacologic blockade of FAK autophosphorylation decreases human glioblastoma tumor growth and synergizes with temozolomide. Mol Cancer Ther. 2013 Feb;12(2):162-72. doi: 10.1158/1535-7163.MCT-12-0701. PubMed PMID: 23243059; PubMed Central PMCID: PMC3570595.

13: Caspari T, Hilditch V. Two Distinct Cdc2 Pools Regulate Cell Cycle Progression and the DNA Damage Response in the Fission Yeast S.pombe. PLoS One. 2015 Jul 1;10(7):e0130748. doi: 10.1371/journal.pone.0130748. PubMed PMID: 26131711; PubMed Central PMCID: PMC4488491.

14: O'Connell MJ, Raleigh JM, Verkade HM, Nurse P. Chk1 is a wee1 kinase in the G2 DNA damage checkpoint inhibiting cdc2 by Y15 phosphorylation. EMBO J. 1997 Feb 3;16(3):545-54. PubMed PMID: 9034337; PubMed Central PMCID: PMC1169658.

15: Ayeni JO, Varadarajan R, Mukherjee O, Stuart DT, Sprenger F, Srayko M, Campbell SD. Dual phosphorylation of cdk1 coordinates cell proliferation with key developmental processes in Drosophila. Genetics. 2014 Jan;196(1):197-210. doi: 10.1534/genetics.113.156281. PubMed PMID: 24214341; PubMed Central PMCID: PMC3872185.

16: Gay A, Culliford D, Leyland K, Arden NK, Bowen CJ. Associations between body mass index and foot joint pain in middle-aged and older women: a longitudinal population-based cohort study. Arthritis Care Res (Hoboken). 2014 Dec;66(12):1873-9. doi: 10.1002/acr.22408. PubMed PMID: 25047683; PubMed Central PMCID: PMC4282113.

17: Beierle EA, Ma X, Stewart J, Nyberg C, Trujillo A, Cance WG, Golubovskaya VM. Inhibition of focal adhesion kinase decreases tumor growth in human neuroblastoma. Cell Cycle. 2010 Mar 1;9(5):1005-15. PubMed PMID: 20160475; PubMed Central PMCID: PMC2855768.

18: Hochwald SN, Nyberg C, Zheng M, Zheng D, Wood C, Massoll NA, Magis A, Ostrov D, Cance WG, Golubovskaya VM. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle. 2009 Aug;8(15):2435-43. PubMed PMID: 19571674; PubMed Central PMCID: PMC4824314.

19: Berry LD, Gould KL. Regulation of Cdc2 activity by phosphorylation at T14/Y15. Prog Cell Cycle Res. 1996;2:99-105. Review. PubMed PMID: 9552387.

20: Heffler M, Golubovskaya VM, Conroy J, Liu S, Wang D, Cance WG, Dunn KB. FAK and HAS inhibition synergistically decrease colon cancer cell viability and affect expression of critical genes. Anticancer Agents Med Chem. 2013 May;13(4):584-94. PubMed PMID: 22934709; PubMed Central PMCID: PMC3625516.