| Identification | Back Directory | [Name]
JNJ-26481585 | [CAS]
875320-29-9 | [Synonyms]
CS-1098
Quisinostat
JNJ-26481585
Quisinostat HClbase
JNJ26481585;JNJ 26481585
Quisinostat (JNJ-26481585)
Quisinostat (JNJ-26481585) 2HCl
N1-(2-(1H-indol-3-yl)ethyl)-N4-(pyridin-4-yl)benzene-1,4-diaMine
N-Hydroxy-2-(4-((((1-methyl-1H-indol-3-yl)methyl)amino)-methyl)piperidin-1-yl)pyrimidine-5-car
N-hydroxy-2-[4-[[(1-methylindol-3-yl)methylamino]methyl]piperidin-1-yl]pyrimidine-5-carboxamide
N-Hydroxy-2-(4-((((1-methyl-1H-indol-3-yl)methyl)amino)-methyl)piperidin-1-yl)pyrimidine-5-carbox
N-Hydroxy-2-(4-((((1-Methyl-1H-indol-3-yl)Methyl)aMino)Methyl)piperidin-1-yl)pyriMidine-5-carboxaMide
N-Hydroxy-2-[4-[[[(1-methyl-1H-indol-3-yl)methyl]amino]methyl]-1-piperidinyl]-5-pyrimidinecarboxamide
5-Pyrimidinecarboxamide, N-hydroxy-2-[4-[[[(1-methyl-1H-indol-3-yl)methyl]amino]methyl]-1-piperidinyl]- | [Molecular Formula]
C21H26N6O2 | [MDL Number]
MFCD17010272 | [MOL File]
875320-29-9.mol | [Molecular Weight]
394.47 |
| Chemical Properties | Back Directory | [density ]
1.35 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥19.2 mg/mL in DMSO | [form ]
Powder | [color ]
Off-white to yellow | [InChI]
InChI=1S/C21H26N6O2/c1-26-14-17(18-4-2-3-5-19(18)26)11-22-10-15-6-8-27(9-7-15)21-23-12-16(13-24-21)20(28)25-29/h2-5,12-15,22,29H,6-11H2,1H3,(H,25,28) | [InChIKey]
PAWIYAYFNXQGAP-UHFFFAOYSA-N | [SMILES]
C1(N2CCC(CNCC3C4=C(N(C)C=3)C=CC=C4)CC2)=NC=C(C(NO)=O)C=N1 |
| Hazard Information | Back Directory | [Uses]
JNJ-26481585 is an HDAC1, HDAC2, HDAC4, HDAC10, and HDAC11 inhibitor. Potent Histone deacetylase inhibitor. | [Definition]
ChEBI: N-hydroxy-2-[4-[[(1-methyl-3-indolyl)methylamino]methyl]-1-piperidinyl]-5-pyrimidinecarboxamide is a member of indoles. | [Biological Activity]
jnj-26481585 is a novel histone deacetylase (hdac) inhibitor that exerts a strong potency towards class i hdac (including hdac1, hdac2 and hdac3), with values of inhibition constant ic50 of 0.11, 0.33 and 4.8 nmol/l respectively, leading to strong anti-proliferative activities (ic50 ranging from 3.1 to 246 nmol/l) against a broad range of cancer cell lines including lung, breast, colon, prostate, brain and overian cancer cell lines. recent study results have shown that jnj-26481585 strongly induce the hdac1-suppressed p21waf1,cip1 promoter in vivo, histone h3 acetylation in tumor tissue and apoptosis in human colon cancer cell lines (both apc wild-type and mutant) in vitro.arts j, king p, mari?n a, floren w, beli?n a, janssen l, pilatte i, roux b, decrane l, gilissen r, hickson i, vreys v, cox e, bol k, talloen w, goris i, andries l, du jardin m, janicot m, page m, van emelen k, angibaud p. jnj-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. clin cancer res. 2009;15(22):6841-6851 | [in vivo]
Quisinostat (40 mg/kg; p.o.; once daily; for 3 days) acts as a potent HDAC1 inhibitor that inhibits p21waf1,cip1 ZsGreen tumors in vivo[1].
?
Quisinostat induces continuous H3 acetylation in tumor tissue in vivo[1].
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Quisinostat (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts[1].
| Animal Model: | NMRI nude mice, with HCT116 colon carcinoma cells xenografts[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection, once daily, for 14 days | | Result: | Strongly inhibited the growth of large pre-established HCT116 colon xenografts. |
| [target]
HDAC1 | [IC 50]
HDAC1: 0.11 nM (IC50); HDAC2: 0.33 nM (IC50); HDAC4: 0.64 nM (IC50); HDAC10: 0.46 nM (IC50); HDAC11: 0.37 nM (IC50); HDAC3: 4.86 nM (IC50); HDAC5: 3.69 nM (IC50); HDAC8: 4.26 nM (IC50); HDAC9: 32.1 nM (IC50); HDAC6: 76.8 nM (IC50); HDAC7: 119 nM (IC50) |
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| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
Moltt Biocem Co., Ltd.
|
| Telephone: |
+86-21-38682181 15900741819 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15856/0_EN.htm |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
D&C Chemicals
|
| Telephone: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|