Product Name :
Cereblon modulator 1
Description:
Cereblon modulator 1 (compound F) is a cereblon (CRBN) E3 ligase modulator. Cereblon modulator 1 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3).
CAS:
1860875-51-9
Molecular Weight:
461.85
Formula:
C22H18ClF2N3O4
Chemical Name:
2-(4-chlorophenyl)-N-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-2,3-dihydro-1H-isoindol-5-yl]methyl-2,2-difluoroacetamide
Smiles :
O=C1CCC(C(=O)N1)N1CC2C=C(CNC(=O)C(F)(F)C3C=CC(Cl)=CC=3)C=CC=2C1=O
InChiKey:
PWBHUSLMHZLGRN-UHFFFAOYSA-N
InChi :
InChI=1S/C22H18ClF2N3O4/c23-15-4-2-14(3-5-15)22(24,25)21(32)26-10-12-1-6-16-13(9-12)11-28(20(16)31)17-7-8-18(29)27-19(17)30/h1-6,9,17H,7-8,10-11H2,(H,26,32)(H,27,29,30)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Cereblon modulator 1 (compound F) is a cereblon (CRBN) E3 ligase modulator. Cereblon modulator 1 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3).|Product information|CAS Number: 1860875-51-9|Molecular Weight: 461.85|Formula: C22H18ClF2N3O4|Chemical Name: 2-(4-chlorophenyl)-N-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-2,3-dihydro-1H-isoindol-5-yl]methyl-2,2-difluoroacetamide|Smiles: O=C1CCC(C(=O)N1)N1CC2C=C(CNC(=O)C(F)(F)C3C=CC(Cl)=CC=3)C=CC=2C1=O|InChiKey: PWBHUSLMHZLGRN-UHFFFAOYSA-N|InChi: InChI=1S/C22H18ClF2N3O4/c23-15-4-2-14(3-5-15)22(24,25)21(32)26-10-12-1-6-16-13(9-12)11-28(20(16)31)17-7-8-18(29)27-19(17)30/h1-6,9,17H,7-8,10-11H2,(H,26,32)(H,27,29,30)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 250 mg/mL (541.Firibastat Biological Activity 30 mM; Need ultrasonic).Maftivimab manufacturer |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:32854124 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|A different CRBN-binding compound, Cereblon modulator 1 (compound F), that demonstrates anti-proliferative activity in non-AML hematological cancer cell lines (such as multiple myeloma) does not inhibit cell growth in any of the 11 AML cell lines tested, including the ten cell lines that are sensitive to the growth inhibitory activity of Compound D. However, when excess Cereblon modulator 1 is added to KG-1 AML cell cultures in the presence of Compound D, the anti-proliferative activity of Compound D is reduced, presumably due to competition for binding of Compound D to CRBN. The relative impact of Cereblon modulator 1 on the anti-proliferative effect of Compound D progressively increased with increasing concentrations of Cereblon modulator 1. In the presence of 100 µΜ Cereblon modulator 1, the potency of Compound D in inhibiting cell growth reduced by approximately 60-fold, and the potency of Compound D in inducing apoptosis reduced by approximately 40-fold.|Products are for research use only. Not for human use.|