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ChemicalBook >> CAS DataBase List >>Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-

Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-

CAS No.
2519823-34-6
Chemical Name:
Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-
Synonyms
BSJ-4-116;BSJ-4-116, 10 mM in DMSO;CDK,degrader,antiproliferative,inhibit,Kelly,C1039F,BSJ 4 116,Cyclin dependent kinase,PROTACs,cancer,Inhibitor,CDK12,mutation,BSJ4116;N-(7-((R)-3-((5-Chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)piperidin-1-yl)heptyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide;Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-
CBNumber:
CB08991762
Molecular Formula:
C40H49ClN8O8S
Molecular Weight:
837.38
MDL Number:
MFCD34186973
MOL File:
2519823-34-6.mol
Last updated:2025-05-10 20:18:10

Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]- Properties

Density 1.368±0.06 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO : 250 mg/mL (298.55 mM; Need ultrasonic)
form Solid
pka 10.68±0.40(Predicted)
color White to off-white

Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]- Chemical Properties,Uses,Production

Uses

BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162)[1].

Biological Activity

BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib [1]. BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F[1].BSJ-4-116 (50 nM; 6-24 hours) decreases the level of CDK12 protein, regardless of the mutational status of the cell line[1].BSJ-4-116 inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition[1]. BSJ-4-116 regulates DDR genes via poly(adenylation). BSJ-4-116 overcomes CDK12C1039F mutation. BSJ-4-116 represents the first example of resistance to a bivalent degrader molecule that is a consequence of an acquired point mutation in the target protein[1].

IC 50

CDK12: 6 nM (IC50); Cereblon

storage

Store at -20°C

References

[1]. Jiang B, et al. Discovery and resistance mechanism of a selective CDK12 degrader. Nat Chem Biol. 2021;17(6):675-683.

Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]- Preparation Products And Raw materials

Raw materials

Preparation Products

Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]- Suppliers

Global( 45)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 33024 60
TargetMol Chemicals Inc. 		+17819995354 marketing@targetmol.com United States 32283 58
InvivoChem 		+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58
Nantong HI-FUTURE Biology Co., Ltd. 		+undefined18051384581 sales@chemhifuture.com China 3135 58
TargetMol Chemicals Inc. 		support@targetmol.com United States 38665 58
LEAPCHEM CO., LTD. 		+86-852-30606658 market18@leapchem.com China 43340 58
Aladdin Scientific 		tp@aladdinsci.com United States 57505 58
Shanghai SuperLan Chemcial Technique Centre 021-2022843681 15618226720 lucy@atkchemical.com China 10123 58
ShangHai Caerulum Pharma Discovery Co., Ltd. 18149758185 18149758185 sales-cpd@caerulumpharma.com China 3474 58
Shanghai Lollane Biological Technology Co.,Ltd. 021-52996696，15000506266 15000506266 China 4621 55

View Lastest Price from Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]- manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
BSJ-4-116 pictures 2025-05-10 BSJ-4-116
2519823-34-6
 US $50.00-189.00 / mg 99.09% 10g TargetMol Chemicals Inc.
  • BSJ-4-116 pictures
  • BSJ-4-116
    2519823-34-6
  • US $50.00-189.00 / mg
  • 99.09%
  • TargetMol Chemicals Inc.
Acetamide, N-[7-[(3R)-3-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]- BSJ-4-116 N-(7-((R)-3-((5-Chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)piperidin-1-yl)heptyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide CDK,degrader,antiproliferative,inhibit,Kelly,C1039F,BSJ 4 116,Cyclin dependent kinase,PROTACs,cancer,Inhibitor,CDK12,mutation,BSJ4116 BSJ-4-116, 10 mM in DMSO 2519823-34-6 C40H49ClN8O8S