2. PROTAC Immunology/Inflammation Apoptosis
  3. PROTACs IRAK Apoptosis
  4. KT-474

KT-474  (Synonyms: KYM-001; PROTAC IRAK4 degrader-7)

Cat. No.: HY-145483 Purity: 98.38%
SDS COA Handling Instructions

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KT-474 (KYM-001) is an orally active PROTAC IRAK4 degrader with antitumor activities. KT-474 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

KT-474 Chemical Structure

KT-474 Chemical Structure

CAS No. : 2432994-31-3

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1 mg USD 300 In-stock
5 mg USD 760 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

KT-474 Related Antibodies

Top Publications Citing Use of Products

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IRAK1 IRAK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

KT-474 (KYM-001) is an orally active PROTAC IRAK4 degrader with antitumor activities[1]. KT-474 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

IRAK4

 

In Vitro

KT-474 (1-100 nM) inhibits Resiquimod (HY-13740)-induced and lipopolysaccharide (HY-D1056)-induced IL-6 and IL-8 production by PBMCs[2].
KT-474 (10-100 nM) inhibits NF-kB activation (phospho-p65) in CpG-B stimulated B cells[2].
KYM-001 (48-72 h) inhibits cell cycle and induces apoptosis in ABC DLBCL, with preferential activity in MYD88-mutant vs MYD88-WT cell lines[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KT-474 Related Antibodies
In Vivo

KT-474 (p.o.) induces tumor regression in xenograft models of MYD88-mutant ABC DLBCL[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

865.93

Formula

C44H49F2N11O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C(CCC2=O)C(N2)=O)C3=CC=CC(C#CCOC(CC4)CCN4C[C@H]5CC[C@@](N(N=C6C(F)F)C=C6NC(C7=C(N=C(N8[C@@H](CO9)C[C@@H]9C8)C=C%10)N%10N=C7)=O)([H])CC5)=C3N1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (115.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1548 mL 5.7741 mL 11.5483 mL
5 mM 0.2310 mL 1.1548 mL 2.3097 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.27%

SDS (393 KB)

COA (254 KB) HNMR (149 KB) LCMS (101 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1548 mL 5.7741 mL 11.5483 mL 28.8707 mL
5 mM 0.2310 mL 1.1548 mL 2.3097 mL 5.7741 mL
10 mM 0.1155 mL 0.5774 mL 1.1548 mL 2.8871 mL
15 mM 0.0770 mL 0.3849 mL 0.7699 mL 1.9247 mL
20 mM 0.0577 mL 0.2887 mL 0.5774 mL 1.4435 mL
25 mM 0.0462 mL 0.2310 mL 0.4619 mL 1.1548 mL
30 mM 0.0385 mL 0.1925 mL 0.3849 mL 0.9624 mL
40 mM 0.0289 mL 0.1444 mL 0.2887 mL 0.7218 mL
50 mM 0.0231 mL 0.1155 mL 0.2310 mL 0.5774 mL
60 mM 0.0192 mL 0.0962 mL 0.1925 mL 0.4812 mL
80 mM 0.0144 mL 0.0722 mL 0.1444 mL 0.3609 mL
100 mM 0.0115 mL 0.0577 mL 0.1155 mL 0.2887 mL
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KT-474 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KT-4742432994-31-3KYM-001 PROTAC IRAK4 degrader-7KT474KT 474KYM001KYM 001PROTACsIRAKApoptosisInterleukin-1 receptor associated kinaseIL-1R associated kinaseantitumororally activeInhibitorinhibitorinhibit

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