KX1-004

Alias: KX1004; KX 1004; KX1-004
Cat No.:V2889 Purity: ≥98%
KX1-004 is a novel and potent small molecule inhibitor of Src-protein tyrosine kinase that can be used to reduce cisplatin ototoxicity while preserving its antitumor effect.
KX1-004 Chemical Structure CAS No.: 518058-84-9
Product category: Src
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
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500mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

KX1-004 is a novel and potent small molecule inhibitor of Src-protein tyrosine kinase that can be used to reduce cisplatin ototoxicity while preserving its antitumor effect. Additionally, KX1-004 has been utilized to shield the cochlea from damaging noise. When compared to control saline treated animals, animals treated with KX1-004 showed an average 10 dB reduction in permanent threshold shift by day 21 and a reduction in temporary threshold shift of 10 to 20 dB at day 1. There were no noteworthy adverse effects associated with the medication treatments, such as appetite loss, weight loss, lethargy, etc. Although at a much lower concentration, KX1-004 provided at least as much protection as L-NAC.

Biological Activity I Assay Protocols (From Reference)
Targets
Src-PTK (IC50 = 40 μM)
ln Vitro

KX1-004 is a novel and potent Src-protein tyrosine kinase inhibitor that can be used to lessen cisplatin ototoxicity without sacrificing its antitumor properties. Additionally, KX1-004 has been used to shield the cochlea from dangerous noise. Compared to control saline treated animals, animals treated with KX1-004 showed an average 10 dB reduction in permanent threshold shift by day 21 and a reduction in temporary threshold shift of 10 to 20 dB at day 1. There were no notable adverse effects associated with the medication treatments, such as appetite loss, weight loss, lethargy, etc. KX1-004 produced protection equivalent to or greater than L-NAC, albeit at a much lower concentration.

ln Vivo
In terms of defense against noise-induced outer hair cell (OHC) loss and temporary and permanent threshold shifts (TTS and PTS), KX1-004 (30 µM) offers substantial protection[1].
KX1-004 (50 mg/kg) is efficient in preventing exposure to noise[2].
Enzyme Assay
One promising medication to prevent NIHL is KX1-004, a strong small molecule inhibitor of Src-PTK.
Animal Protocol
Administered subcutaneously at a dose of 50 mg/kg
N/A
References

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

[2]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H13FN2O2
Molecular Weight
284.10
Exact Mass
284.10
Elemental Analysis
C, 67.60; H, 4.61; F, 6.68; N, 9.85; O, 11.26
CAS #
518058-84-9
Related CAS #
518058-84-9
Appearance
white solid powder
SMILES
C1=CC(=CC(=C1)O)CNC(=O)C2=CC3=C(N2)C=CC(=C3)F
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)
Chemical Name
5-fluoro-N-[(3-hydroxyphenyl)methyl]-1H-indole-2-carboxamide
Synonyms
KX1004; KX 1004; KX1-004
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ≥ 40 mg/mL
Water: <1 mg/mL
Ethanol: N/A
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (8.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.5199 mL 17.5994 mL 35.1989 mL
5 mM 0.7040 mL 3.5199 mL 7.0398 mL
10 mM 0.3520 mL 1.7599 mL 3.5199 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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