AES-135

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AES-135 是一种有效的 HDAC 抑制剂，抑制 HDAC3、HDAC6、HDAC11（IC50：654、190 和 636 nM），具有抗肿瘤活性。

AES-135 is a potent HDAC inhibitor, inhibits HDAC3, HDAC6, HDAC11 (IC50s: 654, 190, and 636 nM) with anti-tumor activity.

AES-135 inhibits cancer cells growth with IC50 values of 2.3 μM, 1.4 μM, 0.27 μM, 0.94 μM, 1.9 μM, 2.72 μM, 2.1 μM, 15.0 μM, 1.6 μM and 19.2 μM for BT143, BT189, D425, D458, MV4-11, MOLM-13, MDA-MB-231, K562, PC-3 and MRC-9 cells, respectively.体:

AES-135 (50 mg/kg; intraperitoneal injection; 5 days a week; for 1 month) treatment significantly increases survival of C57Bl/6 mice implanted with KPC2 cells.NSG mice are dosed with a single 20 mg/kg intraperitoneal (IP) injection, and blood is taken at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h. AES-135 achieved μM concentrations in the blood, reaching Cmax 7452 ng/mL (10.74 μM) within 30 min, which is sustained for 8 h. The blood concentration of AES-135 is dose dependent, achieving an average of 323 ng/mL (0.47 μM) with 10 mg/kg dosing and 1829 ng/mL (2.64 μM) with 40 mg/kg. AES-135 shows an impressive pharmacokinetic profile in mice with an in vivo half-life of 5.0 h. Animal Model:C57Bl/6 mice injected with KPC2 cellsDosage:50 mg/kgAdministration:Intraperitoneal injection; 5 days a week; for 1 monthResult:Significantly increased survival of mice.

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Cell Cycle/DNA Damage

HDAC

HDAC11|HDAC3|HDAC6

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2361659-61-0

693.66

C33H29F6N3O5S

>98% (HPLC)

DMSO:100 mg/mL?(144.16 mM;?Need ultrasonic)

CC(C)(C)C1=CC=C(C=C1)CN(C2=CC=C(C=C2)C(=O)NO)C(=O)CN(CC3=C(C(=C(C(=C3F)F)F)F)F)S(=O)(=O)C4=CC=C(C=C4)F

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(-20℃)

With Ice Pack

≥ 2 years