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]-

Product 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]-
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;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
Formula Weight: 837.38
MOL File: 2519823-34-6.mol

More

Less

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]- Property

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

More

Less

Hazard and Precautionary Statements (GHS)

More

Less

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,Usage,Production

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].

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

More

Less

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

China 27 United States 4 Global 31

Shanghai SuperLan Chemcial Technique Centre

Tel: 021-2022843681 15618226720
Fax: +86-21-51601218
Email: lucy@atkchemical.com
Country: China
ProdList: 9952
Advantage: 58

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3466
Advantage: 58

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4566
Advantage: 55

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8012
Advantage: 62

Shanghai Rechem science Co., Ltd.

Tel: 21-31433387 15618786686
Fax: QQ:1369748377
Email: sales@rechemscience.com
Country: China
ProdList: 2988
Advantage: 58

Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 7296
Advantage: 58

Jilin Province Woda Biotechnology Co., Ltd.

Tel: 13504435624
Email: 1927928688@qq.com
Country: China
ProdList: 1458
Advantage: 58

TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Country: United States
ProdList: 32161
Advantage: 58

InvivoChem

Tel: +1-708-310-1919 +1-13798911105
Fax: 708-557-7486
Email: sales@invivochem.cn
Country: United States
ProdList: 6391
Advantage: 58

DC Chemicals

Tel: 021-58447131 13564518121
Email: sales@dcchemicals.com
Country: China
ProdList: 9409
Advantage: 58

2519823-34-6, 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]-Related Search:

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

2519823-34-6

C40H49ClN8O8S