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| | XY028-133 Basic information |
| Product Name: | XY028-133 | | Synonyms: | XY028-133;L-Prolinamide, N-[7-[4-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]-1,7-dioxoheptyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-;(2S,4R)-1-((S)-2-(7-(4-(6-((6-Acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;(2S,4R)-1-[(2S)-2-(7-{4-[6-({6-acetyl-8-cyclopentyl-5-methyl-7-oxo-7H,8H-pyrido[2,3-d]pyrimidin-2-yl}amino)pyridin-3-yl]piperazin-1-yl}-7-oxoheptanamido)-3,3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}pyrrolidine-2-carboxamide;MS 28 New;XY028-133, 10 mM in DMSO | | CAS: | 2229974-73-4 | | MF: | C53H67N11O7S | | MW: | 1002.23 | | EINECS: | | | Product Categories: | | | Mol File: | 2229974-73-4.mol |  |
| | XY028-133 Chemical Properties |
| density | 1.307±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C, sealed storage, away from moisture and light | | solubility | DMSO : 50 mg/mL (49.89 mM; Need ultrasonic) | | form | Solid | | pka | 14.08±0.40(Predicted) | | color | Light yellow to green yellow |
| | XY028-133 Usage And Synthesis |
| Uses | XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK[1]. | | Biological Activity | XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity[1].
XY028-133 (1 and 3 μM, 24 h) significantly decreases CDK4/6, Cyclin A, PLK1 and pRb protein levels in A375 cells[1]. | | IC 50 | CDK4; CDK6 | | References | [1]. JIN, Jian, et al. COMPOSITIONS AND METHODS FOR TREATING CDK4/6-MEDIATED CANCER. Patent. US2017/065027. |
| | XY028-133 Preparation Products And Raw materials |
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