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HDAC-IN-31

CAS No. : 1916505-13-9

MCE 站：HDAC-IN-31

产品活性：HDAC-IN-31 是一种有效、选择性和具有口服活性的 HDAC 抑制剂，HDAC1、HDAC2、HDAC3、HDAC8 的 IC₅₀ 值分别为 84.90, 168.0, 442.7, >10000 nM。 HDAC-IN-31 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在在 G2/M 期。HDAC-IN-31 显示出良好的抗肿瘤功效。HDAC-IN-31 具有研究弥漫性大B细胞淋巴瘤的潜力。

研究领域：Apoptosis  |  Epigenetics  |  Cell Cycle/DNA Damage

作用靶点：Apoptosis  |  HDAC

In Vitro: HDAC-IN-31 (compound 24g) (2 M) shows growth-inhibitory activities with the inhibition rate of 2.32%, 44.01%, 48.53%, 64.94% for TMD-8, HCT 116, A549, MDA-MB-231 cells.
HDAC-IN-31 (1 M) shows selectivity with the IC₅₀s of 84.9, 168.0, 442.7, >10000 nM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, ａnd 81.20%, 84.43%, 88.07%, 92.34%, 96.88%, 91.98% enzyme activity for HDAC4, HDAC 5,HDAC 7, HDAC9, HDAC 6, HDAC 11, respectively.
HDAC-IN-31 (2.5, 5, 7.5, 10 M; 24 h) increases the expression of HDAC1, Ace-H3, Ace-H4, Cleaved PARP, Cleaved Caspase-3 in a dose-dependent manner.
HDAC-IN-31 (0-4 M; 24 h)induce apoptosis ａnd cell cycle arrests in G2/M phase in a dose-dependent manner.

In Vivo: HDAC-IN-31 (2 mg/kg for i.v.; 10, 100 mg/kg for p.o.) shows good bioavailability with a significant dose dependent manner.
HDAC-IN-31 (50, 100 mg/kg; p.o, daily for 21 consecutive days) shows good antitumor efficacy in a TMD-8 xenograft model without obvious toxicity.
Pharmacokinetic Parameters of HDAC-IN-31 in mice.

Parameters	Unit	24 g (25 mg/kg)
Cmax	nghmL-1	3100±231
T1/2(po)	h	4.4±0.3
AUC0-inf(iv)	nghmL-1	1040±142
AUC0-inf(po)	nghmL-1	5180±252
MRTPO	h	2.6±0.4
F	%	39.9±2.1

ICR mouse; 2 mg/kg for i.v.; 25 mg/kg for p.o..
Pharmacokinetic Parameters of HDAC-IN-31 in tumor models.

Parameters	Unit	po (25 mg/kg)	po (50 mg/kg)	po (100 mg/kg)
Cmax	nghmL-1	1700±317	14700±1024	10700±1001
AUC0-t	nghmL-1	1220±242	9710±314	9740±230
AUC0-inf	nghmL-1	1230±165	9730±341	9770±332
MRT0-t	h	0.750±0.043	0.812±0.023	1.43±0.56
MRT0-inf	h	0.805±0.086	0.821±0.041	1.51±0.32

Mouse; 25, 50, 100 mg/kg for p.o..
Pharmacokinetic Parameters of HDAC-IN-31 in tumor models.

PK parameters	Unit	iv (2 mg/kg)	po (10 mg/kg)	po (100 mg/kg)
Cmax	nghmL-1		3960±413	58300±1352
T1/2	h	0.427±0.016	1.31±0.27	1.63±0.52
AUC0-inf	nghmL-1	1250±132	2670±286	57200±1047
MRT	h	0.402±0.032	0.919±0.052	0.897±0.041
CL	mLkgmin-1	27.2±1.2
F	%		45.6±1.2	91.8±2.3

ICR mice; 2 mg/kg for i.v.; 10, 100 mg/kg for p.o..
Pharmacokinetic Parameters of HDAC-IN-31 in tumor models.

PK parameters	Unit	Monkey		Dog
		iv (1 mg/kg)	po (10 mg/kg)	iv (1 mg/kg)	po (10 mg/kg)
Cmax	nghmL-1		8520±301		4740±243
T1/2	h	4.31±0.56	9.14±0.32	1.65±0.41	1.51±0.33
AUC0-inf	nghmL-1	15700±1842	53200±1241	2550±365	15100±2004
MRT	h	3.41±0.12	8.28±0.32	2.26±0.41	2.71±0.32
CL	mLkgmin-1	1.35±0.21		6.72±0.35
Vdss	Lkg-1	0.34±0.22		0.55±0.04
F	%		27.6±2.1		58.9±1.2

Dogs ａnd monkeys; 1 mg/kg for i.v., 10 mg/kg for p.o. for monkey; 1 mg/kg for i.v., 10 mg/kg for p.o. for dog.

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