DC Chemicals Limited
China
Product Name: Quisinostat (JNJ-26481585) 2HCl
Price: $450.0/100mg $800.0/250mg $1700.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: N-HYDROXY-2-(4-((((1-METHYL-1H-INDOL-3-YL)METHYL)AMINO)METHYL)PIPERIDIN-1-YL)PYRIMIDINE-5-CARBOXAMIDE
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

875320-29-9

875320-29-9 structure

875320-29-9 structure

Name: Quisinostat
Chemical Name: N-hydroxy-2-[4-[[(1-methylindol-3-yl)methylamino]methyl]piperidin-1-yl]pyrimidine-5-carboxamide
CAS Number: 875320-29-9
Molecular Formula: C₂₁H₂₆N₆O₂
Molecular Weight: 394.47000
Catalog: Biochemical Inhibitor Epigenetics HDAC inhibitor
Create Date: 2018-12-28 08:46:39
Modify Date: 2024-01-02 16:38:53
Quisinostat (JNJ-26481585) is an orally available, potent HDAC inhibitor with an IC50 of 0.11 nM for HDAC1.

Name	N-hydroxy-2-[4-[[(1-methylindol-3-yl)methylamino]methyl]piperidin-1-yl]pyrimidine-5-carboxamide
Synonyms	Quisinostat [USAN] QUISINOSTAT Quisinostat (USAN/INN) N-Hydroxy-2-(4-((((1-methyl-1H-indol-3-yl)methyl)amino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide S1096_Selleck UNII-9BJ85K1J8S JNJ-26481585

Description	Quisinostat (JNJ-26481585) is an orally available, potent HDAC inhibitor with an IC50 of 0.11 nM for HDAC1.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC Signaling Pathways >> Epigenetics >> HDAC Research Areas >> Cancer
Target	HDAC1:0.11 nM (IC50) HDAC2:0.33 nM (IC50) HDAC11:0.37 nM (IC50) HDAC10:0.46 nM (IC50) HDAC5:3.69 nM (IC50) HDAC8:4.26 nM (IC50) HDAC3:4.86 nM (IC50) HDAC9:32.1 nM (IC50) HDAC6:76.8 nM (IC50) HDAC7:119 nM (IC50)
In Vitro	Quisinostat exerts broad-spectrum antiproliferative activity against a wide panel of cancer cell lines including lung, colon, breast, prostate, and ovarian cell lines at nanomolar concentrations. JNJ-26481585 shows activity toward all HDAC enzymes tested with highest potency in vitro observed toward recombinant HDAC1 (IC50, 0.11±0.03 nM), which is comparable with the potency observed toward HDAC1-immunoprecipitated complexes from tumor cells (IC50, 0.16±0.02 nM). Lowest in vitro potency is observed toward HDAC6, 7 and 9 (IC50, 32.1-119 nM) [1].
In Vivo	JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo. JNJ-26481585, a “second-generation” HDAC inhibitor with prolonged pharmacodynamic response in vivo. In agreement with the hypothesis, JNJ-26481585 showed superior efficacy compared with both standard of care agents and first-generation HDAC inhibitors in preclinical tumor models. These studies suggest that an HDAC inhibitor with continuous pharmacodynamic activity may show activity in solid tumor malignancies[1].
Animal Admin	JNJ-26481585 is dissolved in DMSO as 5mM stock solution and diluted with appropriate medium. Human A2780 ovarian tumor cells (107 cells/mouse) are injected s.c. into the inguinal region of male athymic nu/nu CD-1 mice. When palpable tumors are obtained, mice are treated once daily with vehicle (10% hydroxypropyl-β-cyclodextrin) or JNJ-26481585 at 10 mg/kg i.p., and tumor and plasma is harvested at day 1 and at day 7 at the indicated time points (5 mice/point). Levels of AcH3 are determined using a quantitative ELISA (300 ng tumor protein/well) and described on the basis of an indirect response pharmacodynamic model[1].
References	[1]. Arts J, et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51.

Density	1.358g/cm3
Boiling Point	615.103ºC at 760 mmHg
Molecular Formula	C₂₁H₂₆N₆O₂
Molecular Weight	394.47000
Flash Point	325.803ºC
Exact Mass	394.21200
PSA	95.31000
LogP	2.94030
Index of Refraction	1.688
Storage condition	-20℃

HS Code	2933990090

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%