CPI-1612

COA

级别和纯度:

≥99%

CAS编号: 2374971-81-8
分子式: C₂₇H₂₆N₆O
分子量: 450.53
PubChem编号: 146014965

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货号 (SKU)	包装规格	是否现货
C646560-5mg	5mg	期货
C646560-10mg	10mg	期货
C646560-25mg	25mg	期货
C646560-50mg	50mg	期货
C646560-100mg	100mg	期货

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Histone Acetyltransferase (79) Histone Modification (3105) 表观遗传学 (1497)

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基本描述

规格或纯度	≥99%
英文名称	CPI-1612
生化机理	CPI-1612 是一种高效的口服活性 EP300/CBP 组蛋白乙酰转移酶（HAT）抑制剂，对 EP300 HAT 的 IC 50 为 8.1 nM。CPI-1612 具有抗癌活性。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC 50 of 8.1 nM for EP300 HAT . CPI-1612 has an anticancer activity In Vitro CPI-1612 inhibits full length EP300 and full length CBP with IC 50 values <0.5 nM and 2.9 nM, respectively. ?\nCPI-1612 inhibits H3K18Ac MSD (H3K18 = histone 3 lysine 18, MSD = meso scale discovery) and JEKO-1 cell proliferation with with IC 50 values 14 nM and <7.9 nM, respectively. ?\nCPI-1612 (compound 17) shows weak activity in a hERG binding assay (IC 50 = 10.4 μM) and displayed moderate inhibition of CYP2C8 (IC 50 = 1.9 μM) and CYP2C19 (IC 50 = 2.7 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo CPI-1612 (compound 17; 0.5 mg/kg; oral administration; twice a day; for 4 weeks) treatment shows 67% tumor growth inhibition (TGI) with concomitant reduction of H3K27Ac in plasma and reduction of H3K18Ac in the tumor . ?\nWhile the oral exposure of CPI-1612 (compound 17) in dogs (0.5 mg/kg IV; 1.0 mg/kg PO; clearance = 0.42 L/h/kg, V ss = 3.7 L/kg, T 1/2 = 5.5 h, F% = 71; AUC/dose = 1691 h·mg/mL) and mice (1 mg/kg IV; 5 mg/kg PO; clearance = 3.8 L/h/kg, V ss = 2.0 L/kg, T 1/2 = 0.98 h, F% = 79; AUC/dose = 211 h·mg/mL) is good, the exposure in rats is limited by poor bioavailability (1.0 mg/kg IV; 5.0 mg/kg PO; clearance = 2.6 L/h/kg, V ss = 1.8 L/kg, T 1/2 = 1.2 h, F% = 9; AUC/dose = 35.6 h·mg/mL) . ?\nA single dose of CPI-1612 is administered orally to CD-1 mice and brain and plasma exposures of CPI-1612 are measured at 0.25, 0.5, 1.0, 2.0, 4.0, and 8.0 h. CPI-1612 is highly brain-penetrant, showing a brain-to-plasma ratio of 0.35 after a single oral dose . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57B6 mice injected with JEKO-1 cells Dosage: 0.5 mg/kg Administration: Oral administration; twice a day; for 4 weeks Result: Showed 67% tumor growth inhibition (TGI) at a dose of 0.5 mg/kg. Form:Solid IC50& Target:CBP/p300
纯度	≥99%

关联靶点（人）

EP300 Tchem 组蛋白乙酰转移酶 p300(Histone acetyltransferase p300) (1 活性数据)

点击查看靶蛋白信息： EP300

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

CREBBP Tchem CREB结合蛋白(CREB-binding protein) (1 活性数据)

点击查看靶蛋白信息： CREBBP

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

KCNH2 Tclin HERG (29587 活性数据)

点击查看靶蛋白信息： KCNH2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP2C8 Tchem Cytochrome P450 2C8 (1492 活性数据)

点击查看靶蛋白信息： CYP2C8

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP2D6 Tclin Cytochrome P450 2D6 (33882 活性数据)

点击查看靶蛋白信息： CYP2D6

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP1A2 Tchem Cytochrome P450 1A2 (26471 活性数据)

点击查看靶蛋白信息： CYP1A2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP2C9 Tchem Cytochrome P450 2C9 (32119 活性数据)

点击查看靶蛋白信息： CYP2C9

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP2C19 Tchem Cytochrome P450 2C19 (29246 活性数据)

点击查看靶蛋白信息： CYP2C19

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP3A4 Tclin Cytochrome P450 3A4 (53859 活性数据)

点击查看靶蛋白信息： CYP3A4

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP2B6 Tchem Cytochrome P450 2B6 (1338 活性数据)

点击查看靶蛋白信息： CYP2B6

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

EP300 Tchem Histone acetyltransferase p300 (1259 活性数据)

点击查看靶蛋白信息： EP300

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

KAT2B Tchem Histone acetyltransferase PCAF (884 活性数据)

点击查看靶蛋白信息： KAT2B

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CREBBP Tchem CREB-binding protein (1602 活性数据)

点击查看靶蛋白信息： CREBBP

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

KAT5 Tchem Histone acetyltransferase KAT5 (85 活性数据)

点击查看靶蛋白信息： KAT5

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

KAT6A Tchem Histone acetyltransferase KAT6A (320 活性数据)

点击查看靶蛋白信息： KAT6A

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

KAT7 Tbio Histone acetyltransferase KAT7 (12 活性数据)

点击查看靶蛋白信息： KAT7

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

KAT6B Tchem Histone acetyltransferase KAT6B (12 活性数据)

点击查看靶蛋白信息： KAT6B

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

JeKo-1 (376 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

关联靶点（其它种属）

Mus musculus (284745 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

GCN5 Histone acetyltransferase GCN5 (89 活性数据)

点击查看靶蛋白信息： GCN5

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	未知
IIUPAC Name	(2R)-2-[[(2S)-2-(4-cyanophenyl)propyl]amino]-N-[5-(1-methylpyrazol-4-yl)pyridin-2-yl]-2-phenylacetamide
INCHI	1S/C27H26N6O/c1-19(21-10-8-20(14-28)9-11-21)15-30-26(22-6-4-3-5-7-22)27(34)32-25-13-12-23(16-29-25)24-17-31-33(2)18-24/h3-13,16-19,26,30H,15H2,1-2H3,(H,29,32,34)/t19-,26-/m1/s1
InChi Key	SEDFZSHSBUXKAC-NIYFSFCBSA-N
Smiles	CC(CNC(C1=CC=CC=C1)C(=O)NC2=NC=C(C=C2)C3=CN(N=C3)C)C4=CC=C(C=C4)C#N
Isomeric SMILES	C[C@H](CN[C@H](C1=CC=CC=C1)C(=O)NC2=NC=C(C=C2)C3=CN(N=C3)C)C4=CC=C(C=C4)C#N
PubChem CID	146014965
分子量	450.53

化学和物理性质

溶解性	DMSO : 100 mg/mL (221.96 mM; Need ultrasonic)

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

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