Catalog No. Size 价格库存数量
S4768-2 2mg solid ¥395
售罄
不可用
S4768-10 10mg solid ¥1,580
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不可用

详情描述

BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity.

Product information

CAS Number: 2349356-09-6

Molecular Weight: 832.90

Formula: C43H48N10O8

Chemical Name: N-(4-{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}butyl)-2-{[2-(2, 6-dioxopiperidin-3-yl)-1, 3-dioxo-2, 3-dihydro-1H-isoindol-4-yl]oxy}acetamide

Smiles: CC(=O)C1C(=O)N(C2CCCC2)C2=NC(NC3=CC=C(C=N3)N3CCN(CCCCNC(=O)COC4=CC=CC5=C4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)=NC=C2C=1C

InChiKey: KDMOCOWXLQOXEB-UHFFFAOYSA-N

InChi: InChI=1S/C43H48N10O8/c1-25-30-23-46-43(49-38(30)52(27-8-3-4-9-27)41(59)36(25)26(2)54)47-33-14-12-28(22-45-33)51-20-18-50(19-21-51)17-6-5-16-44-35(56)24-61-32-11-7-10-29-37(32)42(60)53(40(29)58)31-13-15-34(55)48-39(31)57/h7,10-12,14,22-23,27,31H,3-6,8-9,13,15-21,24H2,1-2H3,(H,44,56)(H,48,55,57)(H,45,46,47,49)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (120.06 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BSJ-03-204 (0.0001-100 μM; for 3 or 4 days) has potent anti-proliferative effects on MCL cell lines. BSJ-03-204 (1 μM; for 1 day) potently induces a G1 arrest. BSJ-03-204 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4/6 in WT cells, not IKZF1/3.

References:

  1. Baishan Jiang, et al. Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6. Angew Chem Int Ed Engl. 2019 May 6;58(19):6321-6326.

Products are for research use only. Not for human use.

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