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[CAS NO. 2230273-76-2] Safimaltib
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-139399 |
| Brand: | MCE |
| CAS: | 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 |
Summary
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
DMSO : 125 mg/mL ( 267.48 mM ; Need ultrasonic)
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 |
References
- [1] Virtual meeting delivers first time drug structures
- [2] A Phase 1, First-in-Human, Open-Label Study of the Safety, Pharmacokinetics, and Pharmacodynamics of JNJ-67856633, an Inhibitor of MALT1, in Participants with NHL and CLL
- [3] Abstract 5690: Discovery of JNJ-67856633: A novel, first-in-class MALT1 protease inhibitor for the treatment of B cell lymphomas
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