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A2AAR/HDAC-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
A2AAR/HDAC-IN-1图片
CAS NO:2767560-51-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
A2AAR/HDAC-IN-1 (compound 14c) 是一种口服有效且平衡的A2AAR/HDAC双抑制剂,其对 A2AAR 的Ki为 163.5 nM, 对HDAC1IC50为 145.3 nM。A2AAR/HDAC-IN-1 具有抗癌 (anticancer) 活性。
生物活性

A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balancedA2AAR/HDACdual inhibitor, with aKiof 163.5 nM for A2AAR and anIC50of 145.3 nM forHDAC1. A2AAR/HDAC-IN-1 showsanticanceractivity[1].

IC50& Target

A2AR

163.5 ± 14 nM (Ki)

A1AR

503.3 ± 14 nM (Ki)

hA2B

>10000 nM (Ki)

Adenosine A3receptor

>10000 nM (Ki)

HDAC1

145.3 ± 12 nM (IC50)

HDAC2

240.2 ± 19 nM (IC50)

HDAC3

443.5 ± 27 nM (IC50)

HDAC6

>10000 nM (IC50)

HDAC8

>10000 nM (IC50)

体外研究
(In Vitro)

A2AAR/HDAC-IN-1 (compound 14c) (0-100 μM, 72 h) shows anti-proliferative activities against colon cancer cell lines, CT26 and MC38[1].
A2AAR/HDAC-IN-1 (0-5 μM, 24 h) increases histone acetylation[1].
A2AAR/HDAC-IN-1 shows moderate selectivity against A1AR (3-fold) and no significant binding for A2BAR and A3AR[1].

Cell Proliferation Assay[1]

Cell Line:Colon cancer cell lines (CT26 and MC38)
Concentration:0-100 μM
Incubation Time:72 h
Result:Displayed good cytotoxicity in CT26 and MC38 cells, with GI50values of 0.29 ± 0.03 μM and 0.38 ± 0.03 μM, respectively.

Western Blot Analysis[1]

Cell Line:MC38 mouse colon cancer cells
Concentration:0, 0.1, 1, and 5 μM
Incubation Time:24 h
Result:Increased histone H3 and H4 acetylation in a concentration-dependent manner.
体内研究
(In Vivo)

A2AAR/HDAC-IN-1 (compound 14c) (30 or 60 mg/kg, IP, twice daily for 9 days) shows potent anti-tumor effects in the mouse MC38 xenograft model[1].
A2AAR/HDAC-IN-1 (90 mg/kg, bid; 150 mg/kg, qd; Oral gavage, for 15 days) shows weak tumor suppression[1].
A2AAR/HDAC-IN-1 (5 mg/kg, IV; 20 mg/kg PO or IP; once) shows an overall favorable pharmacokinetic profile[1].

Animal Model:Male ICR mice (6-8 weeks, ~25 g body weight, MC38 colon cancer model)[1]
Dosage:30 or 60 mg/kg
Administration:IP, twice daily for 9 days
Result:Significantly inhibited tumor growth at a dosage of 30 mg/kg (ip, bid), with a tumor growth inhibition (TGI) rate of 68%. At a dosage of 60 mg/kg, the TGI rate was further increased to 85%.
Animal Model:Male ICR mice (6-8 weeks, ~25 g body weight, MC38 colon cancer model)[1]
Dosage:90 mg/kg, bid; 150 mg/kg, qd
Administration:Oral gavage, twice daily (90 mg/kg) or daily (150 mg/kg), for 15 days
Result:Showed only weak tumor suppression even at a dose of 90 mg/kg (po, bid), with inhibition rates of 44%.
Animal Model:Male ICR mice (6-8 weeks, ~25 g body weight)[1]
Dosage:5 mg/kg (IV) and 20 mg/kg (PO, IP)
Administration:Orally, IP, or IV; once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of A2AAR/HDAC-IN-1 in male ICR mice[1].
PK Parameterspo (20 mg/kg)iv (5 mg/kg)ip (20 mg/kg)
Kel(h-1)0.390 ± 0.1871.820 ± 0.3000.844 ± 0.021
t1/2(h)2.24 ± 1.160.389 ± 0.0700.83 ± 0.02
Tmax(h)0.333 ± 0.140.25 ± 0.00
Cmax(ng/mL)3417 ± 16394703 ± 7358411 ± 693
C0(ng/mL)6498 ± 1285
AUC0-t(ng/mL·h)3602 ± 18072098 ± 14310022 ± 931
CL (mL/min/kg)39.3 ± 2.333.5 ± 3.1
2767560-51-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.