KX1-004 | CAS#518058-84-9 | Src-PTK inhibitor

KX1-004
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406540

CAS#: 518058-84-9

Description: KX1-004 is an Src-protein tyrosine kinase inhibitor to reduce cisplatin ototoxicity while preserving its antitumor effect. KX1-004 has been used to protect the cochlea from hazardous noise.

Chemical Structure

KX1-004

CAS# 518058-84-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406540
Name: KX1-004
CAS#: 518058-84-9
Chemical Formula: C16H13FN2O2
Exact Mass: 284.10
Molecular Weight: 284.290
Elemental Analysis: C, 67.60; H, 4.61; F, 6.68; N, 9.85; O, 11.26

Price and Availability

Size	Price	Availability	Quantity
100mg	USD 750
200mg	USD 1250
500mg	USD 1950
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

More Info:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	KX1-004 is a potent and non-ATP competitive Src-PTK inhibitor with an IC50 of 40 μM.
In vitro activity:	TBD
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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	30.0	105.53
	DMSO	59.0	207.53
	Ethanol	15.8	55.40

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 vitro protocol:	TBD
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.

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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.

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