2. Cell Cycle/DNA Damage Epigenetics GPCR/G Protein
  3. HDAC Adenosine Receptor
  4. A2AAR/HDAC-IN-1

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 HDAC1 的 IC50 为 145.3 nM。A2AAR/HDAC-IN-1 具有抗癌 (anticancer) 活性。

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A2AAR/HDAC-IN-1 Chemical Structure

A2AAR/HDAC-IN-1 Chemical Structure

CAS No. : 2767560-51-8

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A2AAR/HDAC-IN-1 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Adenosine Receptor 亚型特异性产品:

查看所有亚型
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity[1].

IC50 & Target

A2AR

163.5 ± 14 nM (Ki)

A1AR

503.3 ± 14 nM (Ki)

hA2B

>10000 nM (Ki)

Adenosine A3 receptor

>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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CT26 GI50
0.38 μM
Compound: 14c
Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay
[PMID: 35390714]
MC-38 GI50
0.29 μM
Compound: 14c
Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay
[PMID: 35390714]
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

A2AAR/HDAC-IN-1 相关抗体:

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 GI50 values 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 Parameters po (20 mg/kg) iv (5 mg/kg) ip (20 mg/kg)
Kel (h-1) 0.390 ± 0.187 1.820 ± 0.300 0.844 ± 0.021
t1/2 (h) 2.24 ± 1.16 0.389 ± 0.070 0.83 ± 0.02
Tmax (h) 0.333 ± 0.14 0.25 ± 0.00
Cmax (ng/mL) 3417 ± 1639 4703 ± 735 8411 ± 693
C0 (ng/mL) 6498 ± 1285
AUC0-t (ng/mL·h) 3602 ± 1807 2098 ± 143 10022 ± 931
CL (mL/min/kg) 39.3 ± 2.3 33.5 ± 3.1
分子量

439.47

Formula

C24H21N7O2
CAS 号
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.
纯度 & 产品资料
参考文献

A2AAR/HDAC-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

A2AAR/HDAC-IN-12767560-51-8HDACAdenosine ReceptorHistone deacetylasesP1 receptorBifunctionalCancerImmunotherapyCT26MC38colon cancerInhibitorinhibitorinhibit

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