Synonym
KX1004; KX 1004; KX1-004.
IUPAC/Chemical Name
5-fluoro-N-(3-hydroxybenzyl)-1H-indole-2-carboxamide.
InChi Key
TUIHIKXCMCXXJG-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H13FN2O2/c17-12-4-5-14-11(7-12)8-15(19-14)16(21)18-9-10-2-1-3-13(20)6-10/h1-8,19-20H,9H2,(H,18,21)
SMILES Code
O=C(C(N1)=CC2=C1C=CC(F)=C2)NCC3=CC=CC(O)=C3
Appearance
white 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
Biological target:
KX1-004 is a potent and non-ATP competitive Src-PTK inhibitor with an IC50 of 40 μM.
In vivo activity:
Chinchillas were pre-treated with a local administration of pifithrin alpha or KX1-004 and exposed to impulse noise. KX1-004 and pifithrin alpha both decreased threshold shift and the number of missing outer hair cells.
Reference: Neurosci Res. 2014 Apr-May;81-82:30-7. https://pubmed.ncbi.nlm.nih.gov/24472721/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
30.0 |
105.53 |
| DMSO |
59.0 |
207.53 |
| Ethanol |
15.8 |
55.40 |
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
284.29
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:
1. Fetoni AR, Bielefeld EC, Paludetti G, Nicotera T, Henderson D. A putative role of p53 pathway against impulse noise induced damage as demonstrated by protection with pifithrin-alpha and a Src inhibitor. Neurosci Res. 2014 Apr-May;81-82:30-7. doi: 10.1016/j.neures.2014.01.006. Epub 2014 Jan 25. PMID: 24472721.
2. Bielefeld EC, Wantuck R, Henderson D. Postexposure treatment with a Src-PTK inhibitor in combination with N-l-acetyl cysteine to reduce noise-induced hearing loss. Noise Health. 2011 Jul-Aug;13(53):292-8. doi: 10.4103/1463-1741.82962. PMID: 21768733.
In vivo protocol:
1. Fetoni AR, Bielefeld EC, Paludetti G, Nicotera T, Henderson D. A putative role of p53 pathway against impulse noise induced damage as demonstrated by protection with pifithrin-alpha and a Src inhibitor. Neurosci Res. 2014 Apr-May;81-82:30-7. doi: 10.1016/j.neures.2014.01.006. Epub 2014 Jan 25. PMID: 24472721.
2. Bielefeld EC, Wantuck R, Henderson D. Postexposure treatment with a Src-PTK inhibitor in combination with N-l-acetyl cysteine to reduce noise-induced hearing loss. Noise Health. 2011 Jul-Aug;13(53):292-8. doi: 10.4103/1463-1741.82962. PMID: 21768733.
1: Fetoni AR, Bielefeld EC, Paludetti G, Nicotera T, Henderson D. A putative role of p53 pathway against impulse noise induced damage as demonstrated by protection with pifithrin-alpha and a Src inhibitor. Neurosci Res. 2014 Apr-May;81-82:30-7. doi: 10.1016/j.neures.2014.01.006. Epub 2014 Jan 25. PubMed PMID: 24472721.
2: Bielefeld EC, Tanaka C, Chen GD, Coling D, Li M, Henderson D, Fetoni AR. An Src-protein tyrosine kinase inhibitor to reduce cisplatin ototoxicity while preserving its antitumor effect. Anticancer Drugs. 2013 Jan;24(1):43-51. doi: 10.1097/CAD.0b013e32835739fd. PubMed PMID: 22828384.
3: Bielefeld EC, Hangauer D, Henderson D. Protection from impulse noise-induced hearing loss with novel Src-protein tyrosine kinase inhibitors. Neurosci Res. 2011 Dec;71(4):348-54. doi: 10.1016/j.neures.2011.07.1836. Epub 2011 Aug 5. PubMed PMID: 21840347; PubMed Central PMCID: PMC3210387.
4: Bielefeld EC, Wantuck R, Henderson D. Postexposure treatment with a Src-PTK inhibitor in combination with N-l-acetyl cysteine to reduce noise-induced hearing loss. Noise Health. 2011 Jul-Aug;13(53):292-8. doi: 10.4103/1463-1741.82962. PubMed PMID: 21768733.
5: Bielefeld EC, Hynes S, Pryznosch D, Liu J, Coleman JK, Henderson D. A comparison of the protective effects of systemic administration of a pro-glutathione drug and a Src-PTK inhibitor against noise-induced hearing loss. Noise Health. 2005 Oct-Dec;7(29):24-30. PubMed PMID: 17478966.
6: Harris KC, Hu B, Hangauer D, Henderson D. Prevention of noise-induced hearing loss with Src-PTK inhibitors. Hear Res. 2005 Oct;208(1-2):14-25. Epub 2005 Jun 13. PubMed PMID: 15950415.
