2417408-46-7
2417408-46-7 structure
- Name: YX-2-107
- Chemical Name: YX-2-107
- CAS Number: 2417408-46-7
- Molecular Formula: C45H51N11O9
- Molecular Weight: 889.971
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2022-07-01 19:00:27
- Modify Date: 2024-04-09 11:00:12
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YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.
| Name | YX-2-107 |
|---|
| Description | YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib. |
|---|---|
| References | 1. Marco De Dominici, et al. Blood. 2020 Apr 30;135(18):1560-1573. |
| Molecular Formula | C45H51N11O9 |
|---|---|
| Molecular Weight | 889.971 |