2. PROTAC Cell Cycle/DNA Damage
  3. Molecular Glues NEKs
  4. ABS-752 hydrochloride

ABS-752 是一种具有口服活性的靶向 CRBN 调节分子胶 (molecular glue) 的前药。ABS-752 能有效降解 GSPT1。ABS-752 可以降解 NEK7。ABS-752 不与 CRBN 和新底物形成三元复合物。ABS-752 是一种前药，经单胺氧化酶 VAP-1 激活后生成醛中间体，随后转化为活性分子 ABT-002。ABS-752 可用于肝细胞癌 (HCC) 的研究。

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ABS-752 hydrochloride

ABS-752 hydrochloride Chemical Structure

CAS No. : 2922884-90-8

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Other Forms of ABS-752 hydrochloride:

ABS-752 hydrochloride 相关抗体

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NEK1 NEK2 NEK6 NEK7

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ABS-752 is an orally active prodrug of CRBN-modulating molecular glue targeting. ABS-752 can effectively degrade GSPT1. ABS-752 can degrade NEK7. ABS-752 does not form ternary complexes with CRBN and the neosubstrates. ABS-752 is a prodrug activated by the monoamine oxidase, VAP-1, to an aldehyde intermediate and subsequently to the active molecule, ABT-002. ABS-752 can be used for the study of hepatocellular carcinoma (HCC)[1].

IC50 & Target[1]

NEK7

 

GSPT1

 

体外研究
(In Vitro)

ABS-752 (6-24 小时) 可降解 Hep3B 细胞中的 GSPT1、NEK7 和 CK1α，以及 Kelly 细胞中的 SALL4，但不会降解 H929 细胞中的 IKZF1[1]。
ABS-752 (0.01-10 μM，48-72 小时) 主要通过 GSPT1 对 Hep3B 细胞发挥细胞毒性[1]。
ABS-752 (0.1-10 μM，24 小时) 可诱导 Hep3B 野生型细胞中 NEK7 的降解，且该降解现象在 G575N 突变体中仍然存在[1]。
PXS-4728A 可消除 ABS-752 (0.1 nM-30 μM，72 小时) 在 Hep3B 和 KG-1 细胞系中的活性及其对靶蛋白的下调作用[1]。
ABS-752 (0.1 nM-30 μM，72 小时) 在添加 FBS 的培养基中显著降低了 Hep3B 和 KG-1 细胞的活力，但在添加人血清的培养基中则没有这种效果[1]。

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

ABS-752 hydrochloride 相关抗体:

Western Blot Analysis[1]

Cell Line: Hep3B cells, G575N mutant Hep3B cells
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: 48 h
Result: In G575N mutant Hep3B cells, GSPT1 is not degraded; however, in wild-type Hep3B cells, GSPT1 is effectively degraded.
体内研究
(In Vivo)

ABS-752 (1-10 mg/kg, p.o., twice daily for 14 days) exhibits potent antitumor activity in a Hep3B cell xenograft mouse model and degraded GSPT1 and NEK7 in tumor tissue[1].
ABS-752 (100 mg/kg, p.o., twice daily for 20-21 days) effectively inhibits tumor growth in a human hepatocellular carcinoma patient-derived liver cancer xenograft mouse model[1].

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

Animal Model: Female NSG mice subcutaneously implanted with Hep3B human liver cancer cell line[1].
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: P.o., twice daily for 14 days
Result: The 10 mg/kg group showed complete tumor regression.
The 3 mg/kg and 1 mg/kg groups showed significant and moderate tumor growth inhibition, respectively.
GSPT1 and NEK7 degradation was observed in the tumor samples.
Animal Model: 10 Subcutaneous patient-derived liver cancer xenograft (PDX) models were developed in female BALB/c nude mice[1].
Dosage: 100 mg/kg
Administration: P.o., twice daily for 20-21 days
Result: Of the 10 PDX models, 8 showed tumor growth inhibition, with 4 of them having a TGI >50%.
分子量

327.74

Formula

C14H15ClFN3O3
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

ABS-752 hydrochloride 相关分类

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Keywords:

ABS-7522922884-90-8ABS752ABS 752Molecular GluesNEKsNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesTargeted Protein DegradationTPDABT-002GSPT1NEK7Inhibitorinhibitorinhibit

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