CAS 518058-84-9|KX1-004

Introduction：Basic information about CAS 518058-84-9|KX1-004, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. KX1-004 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	KX1-004
CAS Number	518058-84-9	Molecular Weight	284.29
Density	1.4±0.1 g/cm3	Boiling Point	628.2±50.0 °C at 760 mmHg
Molecular Formula	C₁₆H₁₃FN₂O₂	Melting Point	/
MSDS	/	Flash Point	333.7±30.1 °C

Names

Name	1H-Indole-2-carboxamide, 5-fluoro-N-[(3-hydroxyphenyl)methyl]-
Synonym	More Synonyms

KX1-004 BiologicalActivity

Description	KX1-004 is a potent small molecule inhibitor of Src-PTK as a potential protective drug for NIHL.IC50 value:Target: Src-PTK inhibitorKX1-004, KX1-005 and KX1-174 as potential protective drugs for NIHL. Chinchillas were used as subjects. A 30 microl drop of one of the Src inhibitors was placed on the round window membrane of the anesthetized chinchilla; the vehicle (DMSO and buffered saline) alone was placed on the other ear. After the drug application, the middle ear was sutured and the subjects were exposed to noise. Hearing was measured before and several times after the noise exposure and treatment using evoked responses. At 20 days post-exposure, the animals were anesthetized their cochleae extracted and cochleograms were constructed. All three Src inhibitors provided protection from a 4 h, 4 kHz octave band noise at 106 dB. The most effective drug, KX1-004 was further evaluated by repeating the exposure with different doses, as well as, substituting an impulse noise exposure [1]. LNAC was delivered intraperitoneally at a dose of 325 mg/kg while KX1-004 was administered subcutaneously at a dose of 50 mg/kg. The noise exposure consisted of a 4 kHz octave band of noise at 100 dB SPL for 6 hours/day for 4 days. The drugs were administered once each day, 30 minutes prior to the onset of the noise exposure. The animals' hearing was estimated using the evoked response records from surgically-implanted chronic electrodes in the inferior colliculi. Animals treated with LNAC and KX1-004 had from 10 to 20 dB less temporary threshold shift at day 1 and an average 10 dB less permanent threshold shift by day 21 when compared to control saline treated animals [2].
Related Catalog	Signaling Pathways >>Protein Tyrosine Kinase/RTK >>SrcResearch Areas >>Others
References	[1]. Harris KC, et al. Prevention of noise-induced hearing loss with Src-PTK inhibitors. Hear Res. 2005 Oct;208(1-2):14-25. [2]. Bielefeld EC, et al. 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.

Description

KX1-004 is a potent small molecule inhibitor of Src-PTK as a potential protective drug for NIHL.IC50 value:Target: Src-PTK inhibitorKX1-004, KX1-005 and KX1-174 as potential protective drugs for NIHL. Chinchillas were used as subjects. A 30 microl drop of one of the Src inhibitors was placed on the round window membrane of the anesthetized chinchilla; the vehicle (DMSO and buffered saline) alone was placed on the other ear. After the drug application, the middle ear was sutured and the subjects were exposed to noise. Hearing was measured before and several times after the noise exposure and treatment using evoked responses. At 20 days post-exposure, the animals were anesthetized their cochleae extracted and cochleograms were constructed. All three Src inhibitors provided protection from a 4 h, 4 kHz octave band noise at 106 dB. The most effective drug, KX1-004 was further evaluated by repeating the exposure with different doses, as well as, substituting an impulse noise exposure [1]. LNAC was delivered intraperitoneally at a dose of 325 mg/kg while KX1-004 was administered subcutaneously at a dose of 50 mg/kg. The noise exposure consisted of a 4 kHz octave band of noise at 100 dB SPL for 6 hours/day for 4 days. The drugs were administered once each day, 30 minutes prior to the onset of the noise exposure. The animals' hearing was estimated using the evoked response records from surgically-implanted chronic electrodes in the inferior colliculi. Animals treated with LNAC and KX1-004 had from 10 to 20 dB less temporary threshold shift at day 1 and an average 10 dB less permanent threshold shift by day 21 when compared to control saline treated animals [2].

Related Catalog

Signaling Pathways >>Protein Tyrosine Kinase/RTK >>SrcResearch Areas >>Others

References

[1]. Harris KC, et al. Prevention of noise-induced hearing loss with Src-PTK inhibitors. Hear Res. 2005 Oct;208(1-2):14-25.

[2]. Bielefeld EC, et al. 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.

Chemical & Physical Properties

Density	1.4±0.1 g/cm3
Boiling Point	628.2±50.0 °C at 760 mmHg
Molecular Formula	C₁₆H₁₃FN₂O₂
Molecular Weight	284.29
Flash Point	333.7±30.1 °C
PSA	78.88000
LogP	3.30
Appearance of Characters	white solid
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.689
InChIKey	TUIHIKXCMCXXJG-UHFFFAOYSA-N
SMILES	O=C(NCc1cccc(O)c1)c1cc2cc(F)ccc2[nH]1
Storage condition	-20℃

Synonyms

5-Fluoro-N-(3-hydroxybenzyl)-1H-indole-2-carboxamide

KX1-004

Recommended......