2349356-09-6
Chemical Structure
BSJ-03-204
- CAS 番号: 2349356-09-6
- Formula:C43H48N10O8
- Molecular Weight:832.90
IUPAC Name: N-(4-(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)butyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide
InChIKey: KDMOCOWXLQOXEB-UHFFFAOYSA-N
SMILES: O=C1N(C2CCCC2)C3=NC(NC4=CC=C(N(CC5)CCN5CCCCNC(COC6=C(C(N7C(CCC8=O)C(N8)=O)=O)C(C7=O)=CC=C6)=O)C=N4)=NC=C3C(C)=C1C(C)=O
Biological Activity: BSJ-03-204 is a PROTAC-based CDK degrader derived from Palbociclib (HY-50767). BSJ-03-204 targets bovine CDK4/CCND1 and CDK6/CCND1 complexes with IC50 values of 26.9 nM and 10.4 nM, respectively. BSJ-03-204 also triggers ubiquitination and degradation of RB1, reduces pRb levels, thereby inducing G1 cell cycle arrest and exerting antiproliferative effects, as well as inducing time-dependent KLHL8 accumulation. BSJ-03-204 can be used in research related to pancreatic ductal adenocarcinoma, breast cancer, lung cancer, mantle cell lymphoma, and cloned bovine placental hyperplasia[1][2][3][4].
| 製品番号 | 製品名 | 純度 | 製品説明 | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
BSJ-03-204 | 99.76% | BSJ-03-204 is a PROTAC-based CDK degrader derived from Palbociclib (HY-50767). BSJ-03-204 targets bovine CDK4/CCND1 and CDK6/CCND1 complexes with IC50 values of 26.9 nM and 10.4 nM, respectively. BSJ-03-204 also triggers ubiquitination and degradation of RB1, reduces pRb levels, thereby inducing G1 cell cycle arrest and exerting antiproliferative effects, as well as inducing time-dependent KLHL8 accumulation. BSJ-03-204 can be used in research related to pancreatic ductal adenocarcinoma, breast cancer, lung cancer, mantle cell lymphoma, and cloned bovine placental hyperplasia. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Chernobrovkin AL, et al. A Tale of Two Tails: Efficient Profiling of Protein Degraders by Specific Functional and Target Engagement Readouts. SLAS discovery : advancing life sciences R & D. 2021 Apr;26(4):534-546.
- [2]. Kumarasamy V, et al. PROTAC-mediated CDK degradation differentially impacts cancer cell cycles due to heterogeneity in kinase dependencies. British journal of cancer. 2023 Oct;129(8):1238-1250.
- [3]. Jiang B, Wang E S, Donovan K A, et al. Development of dual and selective degraders of cyclin‐dependent kinases 4 and 6[J]. Angewandte Chemie International Edition, 2019, 58(19): 6321-6326.
- [4]. Wu SS, et al. Transcription coactivator YAP1 promotes CCND1/CDK6 expression, stimulating cell proliferation in cloned cattle placentas. Zoological research. 2025 Jan 18;46(1):122-138.
