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voruciclib

CAS编号: 1000023-04-0
分子式: C₂₂H₁₉ClF₃NO₅
分子量: 469.8
PubChem编号: 67409219

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货号 (SKU)	包装规格	是否现货	价格	数量
V614774-5mg	5mg	期货
V614774-25mg	25mg	期货

查看相关系列

casein kinase 1 gamma 1 Inhibitor cyclin dependent kinase 1 Inhibitor cyclin dependent kinase 2 Inhibitor cyclin dependent kinase 4 Inhibitor cyclin dependent kinase 5 Inhibitor cyclin dependent kinase 6 Inhibitor cyclin dependent kinase 8 Inhibitor cyclin dependent kinase 9 Inhibitor dual specificity tyrosine phosphorylation regulated kinase 1B Inhibitor glycogen synthase kinase 3 alpha Inhibitor glycogen synthase kinase 3 beta Inhibitor LIM domain kinase 1 Inhibitor mitogen-activated protein kinase kinase 2 Inhibitor Pim-1 proto-oncogene，serine/threonine kinase Inhibitor

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基本描述

英文名称	voruciclib
别名	P1446A;P1446A-05
英文别名	P1446A;P1446A-05

名称和标识符

IUPAC Name	2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]chromen-4-one
INCHI	InChI=1S/C22H19ClF3NO5/c1-27-5-4-12(14(27)9-28)19-15(29)7-16(30)20-17(31)8-18(32-21(19)20)11-3-2-10(6-13(11)23)22(24,25)26/h2-3,6-8,12,14,28-30H,4-5,9H2,1H3/t12-,14+/m1/s1
InChi Key	MRPGRAKIAJJGMM-OCCSQVGLSA-N
Canonical SMILES	CN1CCC(C1CO)C2=C(C=C(C3=C2OC(=CC3=O)C4=C(C=C(C=C4)C(F)(F)F)Cl)O)O
关联CAS	1000023-04-0
PubChem CID	67409219
MeSH Entry Terms	2-(2-chloro-4-(trifluoromethyl) phenyl)-5, 7-dihydroxy-8-((2R, 3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4H-1-benzopyran-4-one;voruciclib
分子量	469.8

数据库链接

CAS Registry No.	1000023-04-0
PubChem CID	67409219

关联配体

Ligand ID	9923
名称	voruciclib
别名	P1446A
类别	Synthetic organic
学名	2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]chromen-4-one
生物活性评价	Inhibition of kinases other than the CDKs is reported by Paiva et al. (2015) . The observed in vitro inhibition of the GSK3β and PIM1 kinases does not translate to inhibition of these enzymes in CLL cells.
评价	Voruciclib (P1446A, or P1446A-05) is an orally active, non-selective CDK inhibitor that was developed for antineoplastic potential. Potent inhibition of CDK9, 4/6 and 1 by voruciclib is considered as a novel pro-apoptotic mechanism applicable to the treatment of malignant melanoma and to overcome resistance to Bcl-2 inhibition (e.g. by ) in B cell malignancies . Use of voruciclib in combination with BRAF inhibitors for the treatment of malignant melanoma is claimed in patent US20160136132A1 . Preparation of pure (+)-trans enantiomer of the compound shown here, is claimed in patent WO2007148158A1 .

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参考文献

1. Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV. (2015) Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells.. PLoS ONE, 10 (11): (e0143685). [PMID:26606677]
2. Eliades P, Miller DM, Miao B, Kumar R, Taylor M, Buch S, Srinivasa SP, Flaherty KT, Tsao H. (2016) A novel multi-CDK inhibitor P1446A-05 restricts melanoma growth and produces synergistic effects in combination with MAPK pathway inhibitors.. Cancer Biol Ther, 17 (7): (778-84). [PMID:26810603]
3. Dey J, Deckwerth TL, Kerwin WS, Casalini JR, Merrell AJ, Grenley MO, Burns C, Ditzler SH, Dixon CP, Beirne E et al.. (2017) Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition.. Sci Rep, 7 (1): (18007). [PMID:29269870]

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