YX-2-107
Modify Date: 2024-04-09 11:00:12
YX-2-107 structure
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Common Name | YX-2-107 | ||
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| CAS Number | 2417408-46-7 | Molecular Weight | 889.971 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C45H51N11O9 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of YX-2-107YX-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. |
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| References | 1. Marco De Dominici, et al. Blood. 2020 Apr 30;135(18):1560-1573. |
| Molecular Formula | C45H51N11O9 |
|---|---|
| Molecular Weight | 889.971 |