NVP-LCQ195

Modify Date: 2024-07-19 20:13:08

NVP-LCQ195 structure	Common Name	NVP-LCQ195
	CAS Number	902156-99-4	Molecular Weight	460.33500
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₇H₁₉Cl₂N₅O₄S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of NVP-LCQ195

NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.IC50 Value: 1 nM(CDK5/p25 and CDK5/p35); 2 nM(CDK1/cyclinB and CDK2/cyclinA); 5 nM(CDK2/cyclinE); 42 nM(CDK3/cyclinE)Target: CDKsLCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-lmol/l concentrations, spared non-malignant cells, and overcame the protection conferred to MM cells by stroma or cytokines of the bone marrow milieu. In MM cells, LCQ195 triggered decreased amplitude of transcriptional signatures associated with oncogenesis, drug resistance and stem cell renewal, including signatures of activation of key transcription factors for MM cells e.g. myc, HIF-1a, IRF4. Bortezomib-treated MM patients whose tumours had high baseline expression of genes suppressed byLCQ195 had significantly shorter progression-free and overall survival than those with low levels of these transcripts in their MM cells. These observations provide insight into the biological relevance of multi-targeted CDK inhibition in MM.

Name	4-[(2,6-dichlorobenzoyl)amino]-N-(1-methylsulfonylpiperidin-4-yl)-1H-pyrazole-5-carboxamide
Synonym	More Synonyms

Description	NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.IC50 Value: 1 nM(CDK5/p25 and CDK5/p35); 2 nM(CDK1/cyclinB and CDK2/cyclinA); 5 nM(CDK2/cyclinE); 42 nM(CDK3/cyclinE)Target: CDKsLCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-lmol/l concentrations, spared non-malignant cells, and overcame the protection conferred to MM cells by stroma or cytokines of the bone marrow milieu. In MM cells, LCQ195 triggered decreased amplitude of transcriptional signatures associated with oncogenesis, drug resistance and stem cell renewal, including signatures of activation of key transcription factors for MM cells e.g. myc, HIF-1a, IRF4. Bortezomib-treated MM patients whose tumours had high baseline expression of genes suppressed byLCQ195 had significantly shorter progression-free and overall survival than those with low levels of these transcripts in their MM cells. These observations provide insight into the biological relevance of multi-targeted CDK inhibition in MM.
Related Catalog	Research Areas >> Cancer
Target	Cdk5/p25:1 nM (IC50) CDK5/p35:1 nM (IC50) Cdk1/cyclin B:2 nM (IC50) cdk2/cyclin A:2 nM (IC50) CDK2/cyclinE:5 nM (IC50) CDK9/cyclinT1:15 nM (IC50) CDK3/Cyclin E:42 nM (IC50) cdk6/cyclin D3:187 nM (IC50) CDK7/Cyclin H/MAT1:3564 nM (IC50)
References	[1]. McMillin DW, Delmore J, Negri J et al. Molecular and cellular effects of multi-targeted cyclin-dependent kinase inhibition in myeloma: biological and clinical implications. Br J Haematol. 2011 Feb;152(4):420-32.

Molecular Formula	C₁₇H₁₉Cl₂N₅O₄S
Molecular Weight	460.33500
Exact Mass	459.05300
PSA	136.13000
LogP	3.91620
Storage condition	-20°C

Methanesulfonyl...

CAS#:124-63-0

~93%

NVP-LCQ195

CAS#:902156-99-4

Literature: ASTEX THERAPEUTICS LIMITED Patent: WO2008/1101 A2, 2008 ; Location in patent: Page/Page column 366-367 ;

4-amino-1H-pyra...

CAS#:902152-86-7

2,6-Dichloroben...

CAS#:4659-45-4

NVP-LCQ195

CAS#:902156-99-4

Literature: ASTEX THERAPEUTICS LIMITED Patent: WO2008/1101 A2, 2008 ; Location in patent: Page/Page column 369-370 ;

1H-Pyrazole-3-c...

CAS#:825619-04-3

1-methanesulfon...

CAS#:741713-99-5

~49%

NVP-LCQ195

CAS#:902156-99-4

Literature: ASTEX THERAPEUTICS LIMITED Patent: WO2007/129066 A1, 2007 ; Location in patent: Page/Page column 97-98 ;

CS-0840

AT 9311

4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)amide

NVP LCQ195

LCQ 195

NVP-LCQ195

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: NVP-LCQ195
Price: Negotiable
Purity: 98.0%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

DC Chemicals Limited
China
Product Name: NVP-LCQ195
Price: $700.0/100mg $1300.0/250mg $2600.0/1g
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: NVP-LCQ195
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

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Price: $337/10mM*1mLinDMSO

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