性能参数

产品名称

AZD5153 6-Hydroxy-2-naphthoic acid

规格

5mg 10mg 25mg 50mg 100mg 200mg 500mg

货号

GOY-Y3894

 含量

>98.00%

CAS

1869912-40-2

别名

N/A

化学名

N/A

分子式

C36H41N7O6

分子量

分子量 667.75

溶解度

DMSO: ≥ 34 mg/mL (50.92 mM)

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. IC50: 1.7 nM (BRD4)[1]

AZD5153 demonstrates a remarkable enhancement in potency for the displacement of full-length BRD4 relative to BD1, with IC50 values of 5.0 nM and 1.6 μM, respectively. AZD5153 potently disrupts BRD4 foci in U2OS cells with an IC50 value of 1.7 nM. AZD5153 efficiently down-regulates MYC protein levels across the cell line panel irrespective of their sensitivity to AZD5153[1].

Administration of AZD5153 leads to tumor stasis or regression in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma. AZD5153 treatment markedly impacts transcriptional programs of MYC, E2F, and mTOR[1].

[1]. Rhyasen GW, et al. AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies. Mol Cancer Ther. 2016 Nov;15(11):2563-2574.

1-(4-联联苯基)乙醇  3562-73-0  2-氯-5-氟苯酚  3827-49-4

2,6-二氯-4-氟苯酚  392-71-2  4-氨基-5-氯-2,1,3-苯并噻二唑  30536-19-7

2,4-二氯-5-氰基嘧啶  3177-24-0  (-)-顺-6,6-二甲基双环[3.1.1]-2-氨甲基  38235-68-6

6-甲氧基-4-二氢色原酮  39513-75-2  4，5-二甲基-1，2-苯二胺  3171-45-7

4-羟基-2-三氟甲基苯腈  320-42-3  3-氯-2甲

S-羧甲基-L-半胱氨酸S-Carboxymethyl-L-cysteine ,99%638-23-31G

N-乙酰-L-谷氨酰胺N-Acetyl-L-Glutamine,≥98%2490-97-35G

一水肌酸Creatine Monohydrate,≥98%6020-87-725G

硫酸-5-羟色胺肌酐Serotonin creatinine sulfate salt mono...61-47-2100MG

亚氨基二乙酸Iminodiacetic acid,98%142-73-425G

PerilloxinPerilloxin (HPLC,≥98%)263249-77-05MG