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PROTAC CDK2/9 Degrader-1

Product Name
PROTAC CDK2/9 Degrader-1
CAS No.
2408641-24-5
Chemical Name
PROTAC CDK2/9 Degrader-1
Synonyms
PROTAC CDK2;PROTAC CDK2/9 Degrader-1;4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-(4-((2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)amino)-4-oxobutanoyl)piperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide;N-{4-[(4-{3-[(2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}ethyl)carbamoyl]propanoyl}piperazin-1-yl)methyl]phenyl}-4-({7H-pyrrolo[2,3-d]pyrimidin-4-yl}amino)-1H-pyrazole-3-carboxamide
CBNumber
CB28054502
Molecular Formula
C40H41N13O7
Formula Weight
815.84
MOL File
Mol file
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PROTAC CDK2/9 Degrader-1 Property

Density 
1.534±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 130 mg/mL (159.34 mM; Need ultrasonic)
form 
Solid
pka
10.74±0.40(Predicted)
color 
White to yellow
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Hazard and Precautionary Statements (GHS)

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PROTAC CDK2/9 Degrader-1 Chemical Properties,Usage,Production

Biological Activity

PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 μM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand[1]. PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase[1].PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells[1].PROTAC CDK2/9 Degrader-1 effectively degrades CDK2/9 in cell lines MCF-7, HCT-116 and 22Rv1, which all have high CDK2/9 expression[1].PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC50 as 7.42 nM and 14.50 nM, respectively[1].

References

[1]. Zhou F, et al. Development of selective mono or dual PROTAC degrader probe of CDK isoforms. Eur J Med Chem. 2019 Dec 6;187:111952.

PROTAC CDK2/9 Degrader-1 Preparation Products And Raw materials

Raw materials

Preparation Products

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PROTAC CDK2/9 Degrader-1 Suppliers

Jilin Province Woda Biotechnology Co., Ltd.
Tel
13504435624
Email
1927928688@qq.com
Country
China
ProdList
1456
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58
cjbscvictory
Tel
13348960310 13348960310
Email
3003867561@qq.com
Country
China
ProdList
10002
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58
Jilin Chinese Academy of Sciences - Yanshen Technology Co., Ltd
Tel
0431-80514535 19917294565
Email
caoy@chemextension.com
Country
China
ProdList
4755
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58
Changzhou Bojia Biomedical Technology Co., Ltd.
Tel
2122619822
Email
czbjpharma@126.com
Country
China
ProdList
18478
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58
ShenZhen Trendseen Biological Technology Co.,Ltd.
Tel
13417589054 13417589054
Email
trendseenbio@gmail.com
Country
China
ProdList
9470
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58
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd
Tel
021-59167510 18117107507
Email
vip@med-life.cn
Country
China
ProdList
4997
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58

2408641-24-5, PROTAC CDK2/9 Degrader-1Related Search:


  • PROTAC CDK2/9 Degrader-1
  • PROTAC CDK2
  • 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-(4-((2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)amino)-4-oxobutanoyl)piperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide
  • N-{4-[(4-{3-[(2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}ethyl)carbamoyl]propanoyl}piperazin-1-yl)methyl]phenyl}-4-({7H-pyrrolo[2,3-d]pyrimidin-4-yl}amino)-1H-pyrazole-3-carboxamide
  • 2408641-24-5