2. Metabolic Enzyme/Protease NF-κB
  3. MALT1
  4. Safimaltib

Safimaltib  (Synonyms: JNJ-67856633)

Cat. No.: HY-139399 Purity: 99.89%
COA Handling Instructions

Molarity Calculator

Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis.

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

Safimaltib Chemical Structure

Safimaltib Chemical Structure

CAS No. : 2230273-76-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 144 In-stock
Solution
10 mM * 1 mL in DMSO USD 144 In-stock
Solid
5 mg USD 140 In-stock
10 mg USD 230 In-stock
25 mg USD 440 In-stock
50 mg USD 750 In-stock
100 mg USD 1250 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Safimaltib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Safimaltib

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis[1][2][3].

IC50 & Target

MALT1 protease[1][2][3]
In Vitro

Safimaltib (JNJ-67856633) is effective and highly bioavailable in both mouse and rat tumors, and in some cases led to tumor stasis.
Safimaltib leads to potent in vivo pharmacodynamic shutdown in CD79b- as well as CARD11-mutant ABC-DLBCL models as measured by serum IL10 or uncleaved BCL10 levels in tumors[1][3].

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

Safimaltib Related Antibodies
In Vivo

Dose dependent inhibition of the generation of Tregs (CD4+CD25+FoxP3+) following CD3/28 stimulation was observed upon treatment with JNJ-67856633 suggesting a potential immune modulatory role of MALT1 inhibition[3].

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

467.32

Formula

C20H11F6N5O2
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=C(C(F)(F)F)N(C2=CC=CC3=C2C=CNC3=O)N=C1)NC4=CC(C(F)(F)F)=NC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (267.48 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 2.1399 mL 10.6993 mL 21.3986 mL
5 mM 0.4280 mL 2.1399 mL 4.2797 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: ≥ 2.08 mg/mL (4.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: 99.89%

COA (255 KB) HNMR (268 KB) LCMS (261 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 2.1399 mL 10.6993 mL 21.3986 mL 53.4965 mL
5 mM 0.4280 mL 2.1399 mL 4.2797 mL 10.6993 mL
10 mM 0.2140 mL 1.0699 mL 2.1399 mL 5.3497 mL
15 mM 0.1427 mL 0.7133 mL 1.4266 mL 3.5664 mL
20 mM 0.1070 mL 0.5350 mL 1.0699 mL 2.6748 mL
25 mM 0.0856 mL 0.4280 mL 0.8559 mL 2.1399 mL
30 mM 0.0713 mL 0.3566 mL 0.7133 mL 1.7832 mL
40 mM 0.0535 mL 0.2675 mL 0.5350 mL 1.3374 mL
50 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0699 mL
60 mM 0.0357 mL 0.1783 mL 0.3566 mL 0.8916 mL
80 mM 0.0267 mL 0.1337 mL 0.2675 mL 0.6687 mL
100 mM 0.0214 mL 0.1070 mL 0.2140 mL 0.5350 mL
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Safimaltib 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:

Safimaltib2230273-76-2JNJ-67856633JNJ67856633JNJ 67856633MALT1mucosa associated lymphoid tissue lymphoma translocation gene 1orallyactivefirst-in-classpotentselectiveallostericInhibitorinhibitorinhibit

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