ChemicalBook > CAS DataBase List > 4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1)

4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1)

Product Name
4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1)
CAS No.
1000023-05-1
Chemical Name
4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1)
Synonyms
VORUCICLIB HYDROCHLORIDE;4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1)
CBNumber
CB35509251
Molecular Formula
C22H20Cl2F3NO5
Formula Weight
506.3
MOL File
1000023-05-1.mol
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4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1) Property

storage temp. 
4°C, away from moisture
solubility 
DMSO : ≥ 250 mg/mL (493.78 mM)
form 
Solid
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0016536
Product name
Voruciclib(hydrochloride)
Purity
98.20%
Packaging
5mg
Price
$350
Updated
2021/12/16
ChemScene
Product number
CS-0016536
Product name
Voruciclib(hydrochloride)
Purity
98.20%
Packaging
10mg
Price
$550
Updated
2021/12/16
ChemScene
Product number
CS-0016536
Product name
Voruciclib(hydrochloride)
Purity
98.20%
Packaging
50mg
Price
$1650
Updated
2021/12/16
ChemScene
Product number
CS-0016536
Product name
Voruciclib(hydrochloride)
Purity
98.20%
Packaging
100mg
Price
$2250
Updated
2021/12/16
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4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1) Chemical Properties,Usage,Production

Uses

Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL)[1].

in vivo

Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL[1].

Animal Model:ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice[1]
Dosage:200 mpk
Administration:Oral gavage; U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), OCI-LY10 (six days per week for 2 weeks), NU-DHL-1 (five days per week for 3 weeks)
Result:Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model.

IC 50

CDK9/CycT1: 1.68 nM (Ki); CDK9/cyc T2: 0.626 nM (Ki); CDK6/cycD1: 2.92 nM (Ki); CDK4/Cyc D1: 3.96 nM (Ki); CDK1/cycB: 5.4 nM (Ki); CDK1/cyc A: 9.1 nM (Ki)

References

[1] Dey J, et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition. Sci Rep. 2017 Dec 21;7(1):18007. DOI:10.1038/s41598-017-18368-w

4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1) Preparation Products And Raw materials

Raw materials

Preparation Products

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4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1) Suppliers

China 11 United States 2 Global 13
TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767
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Shanghai hongqu biomedical technology co. LTD
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88888888888
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hongquchem@qq.com
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cjbscvictory
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Shanghai Yifei Biotechnology Co. , Ltd.
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RD International Technology Co., Limited
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TargetMol Chemicals Inc.
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Anhui JYHX CO., LTD.
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Biosynth Biological Technology (Suzhou) Co Ltd
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51288865780
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Adooq Bioscience LLC
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1000023-05-1, 4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1)Related Search:

X-082

  • 4H-1-Benzopyran-4-one, 2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1)
  • VORUCICLIB HYDROCHLORIDE
  • 1000023-05-1
  • C22H19ClF3NO5ClH