2078047-99-9
2078047-99-9 structure
- Name: CDDD2-94
- Chemical Name: CDDD2-94
- CAS Number: 2078047-99-9
- Molecular Formula: C21H27FN8S
- Molecular Weight: 442.561
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2022-07-11 16:33:09
- Modify Date: 2024-09-21 19:37:09
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CDDD2-94 is a highly potent and selective CDK4 inhibitor with Ki of 2 nM, >140-fold selective for CDK4 over CDK6 (Ki=279 nM).CDDD2-94 is ineffective against other members of the CDK family, displays high selectivity against a panel of 369 human kinases at 1uM, with exceptionally selective-CLK, DYRKs and MYLK4 were the only kinases targeted potently.CDDD2-94 is the most selective CDK4 inhibitor identified to date.CDDD2-94 demonstrated antiproliferative activityagainst MV4-11 and MDA-MB-453 cell lines with GI50 of 0.107 and 0.325 uM respectively.CDDD2-94 inhibits S780-phosphorylated Rb (pRb(S780)) and decreases transcription of Rb1 and E2F-target genes in MDA-MB-453 cells.CDDD2-94 is well tolerated and efficacious in preclinical OC xenograft model, CDDD2-94 provides better safety profile than palbociclib towards the bone marrow.
| Name | CDDD2-94 |
|---|
| Description | CDDD2-94 is a highly potent and selective CDK4 inhibitor with Ki of 2 nM, >140-fold selective for CDK4 over CDK6 (Ki=279 nM).CDDD2-94 is ineffective against other members of the CDK family, displays high selectivity against a panel of 369 human kinases at 1uM, with exceptionally selective-CLK, DYRKs and MYLK4 were the only kinases targeted potently.CDDD2-94 is the most selective CDK4 inhibitor identified to date.CDDD2-94 demonstrated antiproliferative activityagainst MV4-11 and MDA-MB-453 cell lines with GI50 of 0.107 and 0.325 uM respectively.CDDD2-94 inhibits S780-phosphorylated Rb (pRb(S780)) and decreases transcription of Rb1 and E2F-target genes in MDA-MB-453 cells.CDDD2-94 is well tolerated and efficacious in preclinical OC xenograft model, CDDD2-94 provides better safety profile than palbociclib towards the bone marrow. |
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| References | 1. Laychiluh Bantie, et al. Gynecol Oncol. 2020 Dec;159(3):827-838. 2. Solomon Tadesse, et al. Br J Pharmacol. 2018 Jun;175(12):2399-2413. |
| Molecular Formula | C21H27FN8S |
|---|---|
| Molecular Weight | 442.561 |