Roniciclib

Product Name: Roniciclib
CAS No.: 1223498-69-8
Chemical Name: Roniciclib
Synonyms: Roniciclib;BAY 1000394;BAY1000394 /BAY-1000394;BAY 1000394 (Roniciclib);Roniciclib (BAY 1000394);Roniciclib BAY1000394 BAY-1000394;Roniciclib (Synonyms: BAY 1000394);CDK,Cyclin dependent kinase,BAY-1000394,inhibit,BAY1000394,Roniciclib,Inhibitor;(2R,3R)-3-((2-((4-(cyclopropanesulfonimidoyl)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)oxy)butan-2-ol;(2R,3R)-3-((2-((4-((R)-Cyclopropanesulfonimidoyl)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)oxy)butan-2-ol
CBNumber: CB82658182
Molecular Formula: C18H21F3N4O3S
Formula Weight: 430.44
MOL File: 1223498-69-8.mol

More

Less

Roniciclib Property

Boiling point:: 577.4±60.0 °C(Predicted)
Density: 1.50±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: ≥ 250 mg/mL (580.80 mM)
form: Solid
color: White to off-white

More

Less

Hazard and Precautionary Statements (GHS)

More

Less

N-Bromosuccinimide Price

TRC

Product number: B127600
Product name: BAY1000394
Packaging: 2.5mg
Price: $815
Updated: 2021/12/16

TRC

Product number: B127600
Product name: BAY1000394
Packaging: 5mg
Price: $1525
Updated: 2021/12/16

ChemScene

Product number: CS-0008558
Product name: Roniciclib
Purity: 98.89%
Packaging: 50mg
Price: $2000
Updated: 2021/12/16

ChemScene

Product number: CS-0008558
Product name: Roniciclib
Purity: 98.89%
Packaging: 100mg
Price: $3500
Updated: 2021/12/16

ChemScene

Product number: CS-0008558
Product name: Roniciclib
Purity: 98.89%
Packaging: 5mg
Price: $350
Updated: 2021/12/16

More

Less

Roniciclib Chemical Properties,Usage,Production

Description

Roniciclib is an orally bioavailable cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. Roniciclib selectively binds to and inhibits the activity of CDK1/Cyclin B, CDK2/Cyclin E, CDK4/Cyclin D1, and CDK9/Cyclin T1, serine/threonine kinases that play key roles in the regulation of the cell cycle progression and cellular proliferation. Inhibition of these kinases leads to cell cycle arrest during the G1/S transition, thereby leading to an induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are often dysregulated in cancerous cells.

Uses

BAY 1000394 (Roniciclib)l is a type I pan-CDK inhibitor which is used in xenograft cancer models. Anticancer agent.

in vivo

Tumor growth is strongly inhibited in a dose-dependent manner with T/C values of 0.19 at the lower dose and of 0.02 (tumor regression) at the higher dose. Furthermore, Roniciclib strongly inhibits growth of HeLa-MaTu tumors that have been grown to a size of approximately 50mm² before start of treatment (day 8 after inoculation). Treatment with Roniciclib at doses of 1.5 and 1 mg/kg slow tumor growth to T/C values of 0.15 and 0.62, respectively. Addition of Roniciclib to cisplatin result in a strong tumor growth inhibition with T/C values of 0.01 (1.0 mg/kg Roniciclib) and -0.02 (1.5 mg/kg Roniciclib)^[1].
Roniciclib has low blood clearance rates in mouse, rat, and dog (0.51, 0.78, and 0.50 Lh^-1kg^-1, respectively) ^[2].

IC 50

Cdk1/cyclin B: 7 nM (IC₅₀); CDK2/cyclinE: 9 nM (IC₅₀); CDK4/cyclin D: 11 nM (IC₅₀); CDK9/cyclinT1: 5 nM (IC₅₀); CDK7/Cyclin H/MAT1: 25 nM (IC₅₀)

References

[1] GERHARD SIEMEISTER. BAY 1000394, a novel cyclin-dependent kinase inhibitor, with potent antitumor activity in mono- and in combination treatment upon oral application.[J]. Molecular Cancer Therapeutics, 2012, 11 10: 2265-2273. DOI:10.1158/1535-7163.MCT-12-0286.
[2] DR. ULRICH LÜCKING. The Lab Oddity Prevails: Discovery of Pan-CDK Inhibitor (R)-S-Cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY 1000394) for the Treatment of Cancer[J]. ChemMedChem, 2013, 8 7: 1067-1085. DOI:10.1002/cmdc.201300096.

Roniciclib Preparation Products And Raw materials

Raw materials

Preparation Products

More

Less

Roniciclib Suppliers

China 42 United States 5 Global 47

ShangHai ChuanQian Chemcial Technique Centre

Tel: 15869524721
Email: 3525679403@qq.com
Country: China
ProdList: 4986
Advantage: 58

Jinan Trio PharmaTech Co., Ltd.

Tel: 0531-88811783
Fax: +86 (531) 55696010 QQ 1762738062
Email: sales@trio-pharmatech.com
Country: China
ProdList: 1856
Advantage: 62

NCE Biomedical Co.,Ltd.

Tel: 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax: +86-27-87599188
Country: China
ProdList: 1493
Advantage: 55

AdooQ BioScience, LLC

Tel: +1 (866) 930-6790
Fax: +1 (866) 333-9607
Email: info@adooq.com
Country: United States
ProdList: 2782
Advantage: 58

Sichuan Wei Keqi Biological Technology Co., Ltd.

Tel: 028-81700200 18116577057
Fax: 028-81705658
Email: 3003855609@qq.com
Country: China
ProdList: 7777
Advantage: 56

Suzhou yacoo science co.,Ltd

Tel: 0512-87182056 18013166090
Fax: 0512-87182056
Email: lingling.qi@yacoo.com.cn
Country: China
ProdList: 6295
Advantage: 60

LETOPHARM LIMITED

Tel: +86-21-5821 5861
Fax: +86-21-5106 2861
Email: sales@letopharm.com
Country: China
ProdList: 2384
Advantage: 58

SPIRO PHARMA

Tel
Fax: -
Email: eric_feng1954@126.com
Country: China
ProdList: 9248
Advantage: 55

Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 9505
Advantage: 58

Amadis Chemical Company Limited

Tel: 571-89925085
Fax: 0086-571-89925065
Email: sales@amadischem.com
Country: China
ProdList: 131957
Advantage: 58

1223498-69-8, RoniciclibRelated Search:

BAY 1000394

Roniciclib

BAY 1000394 (Roniciclib)

BAY1000394 /BAY-1000394

Roniciclib (Synonyms: BAY 1000394)

Roniciclib (BAY 1000394)

2-Butanol, 3-[[2-[[4-[[S(R)]-S-cyclopropylsulfonimidoyl]phenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]oxy]-, (2R,3R)-

(2R,3R)-3-((2-((4-(cyclopropanesulfonimidoyl)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)oxy)butan-2-ol

Roniciclib BAY1000394 BAY-1000394

CDK,Cyclin dependent kinase,BAY-1000394,inhibit,BAY1000394,Roniciclib,Inhibitor

(2R,3R)-3-((2-((4-((R)-Cyclopropanesulfonimidoyl)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)oxy)butan-2-ol

1223498-69-8