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Chemical Structure : CDDD2-94
Catalog No.: PC-72637Not For Human Use, Lab Use Only.
CDDD2-94 is a highly potent and selective CDK4 inhibitor with Ki of 2 nM, 140-fold more selective for CDK4 over CDK6 (Ki=279 nM).
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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.
| M.Wt | 442.561 | |
| Formula | C21H27FN8S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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