[CAS NO. 2230273-76-2] Safimaltib

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PRODUCTS SPECIFICATIONS [2230273-76-2]

Catalog

HY-139399

Brand

MCE

CAS

2230273-76-2

DESCRIPTION [2230273-76-2]

Overview

MDL	-
Molecular Weight	467.32
Molecular Formula	C20H11F6N5O2
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

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

Summary

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] .

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

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] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04657224	Janssen Research & Development, LLC	Lymphoma, Non-Hodgkin\|Chronic Lymphocytic Leukemia	February 25, 2021	Phase 1
NCT03900598	Janssen Research & Development, LLC	Leukemia, Lymphocytic, Chronic, B-Cell\|Lymphoma, Non-Hodgkin	April 3, 2019	Phase 1
NCT04876092	Janssen Research & Development, LLC	Leukemia, Lymphocytic, Chronic, B-Cell\|Lymphoma, Non-Hodgkin	July 28, 2021	Phase 1

Appearance

Solid

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)

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
10 mM	0.2140 mL	1.0699 mL	2.1399 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
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
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.