BAY-1143572.

Product Name: BAY-1143572.
CAS No.: 1414943-88-6
Chemical Name: BAY-1143572.
Synonyms: BAY1143572;BAY 1143572;BAY-1143572.;Atuveciclib Racemate;BAY-1143572 Racemate;Atuveciclib(BAY-1143572);Atuveciclib Racemate, 10 mM in DMSO;ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE);1-(4-Fluoro-3-(methylsulfonylmethyl)phenyl)-1H-1,2,4-triazole;4-(4-fluoro-2-methoxyphenyl)-N-(3-((S-methylsulfonimidoyl)methyl)phenyl)-1,3,5-triazin-2-amine
CBNumber: CB03133468
Molecular Formula: C18H18FN5O2S
Formula Weight: 387.43
MOL File: 1414943-88-6.mol

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BAY-1143572. Property

Boiling point:: 589.9±60.0 °C(Predicted)
Density: 1.36±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: 125 mg/mL (322.64 mM)
form: Solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-6307
Product name: AtuveciclibRacemate
Purity: 98.48%
Packaging: 5mg
Price: $550
Updated: 2021/12/16

ChemScene

Product number: CS-6307
Product name: AtuveciclibRacemate
Purity: 98.48%
Packaging: 10mg
Price: $850
Updated: 2021/12/16

DC Chemicals

Product number: DC10376
Product name: BAY-1143572
Purity: >98%
Packaging: 100mg
Price: $950
Updated: 2021/12/16

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BAY-1143572. Chemical Properties,Usage,Production

Uses

Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.

Biological Activity

Atuveciclib (BAY-1143572) is a potent and highly selective PTEFb/CDK9 inhibitor with IC50 of 13 nM for CDK9/CycT. Its IC50 for CDK2 is about 100-fold higher than that for CDK9. In addition to CDK family members, it also inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β, respectively.

in vivo

BAY 1143572 has a low plasma clearance (CL _b 1.1 L/h/kg) and a volume of distribution (Vss) of 1.0 L/kg in a rat pharmacokinetic study . Its oral bioavailability is 54% and the blood-plasma concentration ratio is 1. BAY 1143572 has no significant inhibitory effect on cytochrome P450 activity, IC50>20 μM. NOD/Shi-scid/IL-2Rγ in immunocompromised.

target

Target	Value
CDK9 (Cell-free assay)	13 nM
GSK-3α ()	45 nM
GSK3β ()	87 nM

IC 50

CDK9

References

[1] Scholz A, et al. BAY 1143572, a first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, shows convincing anti-tumor activity in preclinical models of acute myeloid leukemia (AML). [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 3022.
[2] Scholz A, et al. BAY 1143572: A first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, inhibits MYC and shows convincing anti-tumor activity in multiple xenograft models by the induction of apoptosis. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr DDT02-02. doi:10.1158/1538-7445.AM2015-DDT02-02

BAY-1143572. Preparation Products And Raw materials

Raw materials

Preparation Products

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BAY-1143572. Suppliers

China 67 United States 4 USA 1 Global 72

Wuhan Huahan Dingcheng New Material Technology Co., Ltd

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1414943-88-6, BAY-1143572.Related Search:

BAY 1143572

BAY1143572

ATUVECICLIB RACEMATE (BAY-1143572 RACEMATE)

Atuveciclib Racemate

Atuveciclib(BAY-1143572)

(rac)-4-(4-fluoro-2-methoxyphenyl)-N-{3-[(S-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine

4-(4-fluoro-2-methoxyphenyl)-N-(3-((S-methylsulfonimidoyl)methyl)phenyl)-1,3,5-triazin-2-amine

BAY-1143572.

BAY-1143572 Racemate

1,3,5-Triazin-2-amine, 4-(4-fluoro-2-methoxyphenyl)-N-[3-[(S-methylsulfonimidoyl)methyl]phenyl]-

Atuveciclib,BAY1143572,Cyclin dependent kinase,inhibit,Inhibitor,CDK,Atuveciclib Racemate,BAY 1143572,BAY-1143572

Atuveciclib Racemate, 10 mM in DMSO

1-(4-Fluoro-3-(methylsulfonylmethyl)phenyl)-1H-1,2,4-triazole

1414943-88-6