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

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).

For research use only. We do not sell to patients.

ABS-752 hydrochloride

ABS-752 hydrochloride Chemical Structure

CAS No. : 2922884-90-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Other Forms of ABS-752 hydrochloride:

ABS-752 hydrochloride Related Antibodies

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NEK1 NEK2 NEK4 NEK6 NEK7

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Description

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

 

In Vitro

ABS-752 (6-24 h) degrades GSPT1, NEK7, CK1α in Hep3B cells and SALL4 in Kelly cells, but does not degrade IKZF1 in H929 cells[1].
ABS-752 (0.01-10 μM, 48-72 h) exerts its cytotoxicity to Hep3B cells mainly through GSPT1[1].
ABS-752 (0.1-10 μM, 24 h) can induce NEK7 degradation in Hep3B wild-type cells, and this degradation still occurs in the G575N mutant[1].
ABS-752’s (0.1 nM-30 μM, 72 h) activity and target protein downregulation in Hep3B and KG-1 cell lines are abolished by PXS-4728A[1].
ABS-752 (0.1 nM-30 μM, 72 h) significantly reduces Hep3B and KG-1 viability in FBS-supplemented medium, but not in human serum-supplemented medium[1].

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

ABS-752 hydrochloride Related Antibodies

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.
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].

MedChemExpress (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%.
Molecular Weight

327.74

Formula

C14H15ClFN3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=CC(F)=C(CN)C=C2CN1C3C(NC(CC3)=O)=O.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (76.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0512 mL 15.2560 mL 30.5120 mL
5 mM 0.6102 mL 3.0512 mL 6.1024 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0512 mL 15.2560 mL 30.5120 mL 76.2800 mL
5 mM 0.6102 mL 3.0512 mL 6.1024 mL 15.2560 mL
10 mM 0.3051 mL 1.5256 mL 3.0512 mL 7.6280 mL
15 mM 0.2034 mL 1.0171 mL 2.0341 mL 5.0853 mL
20 mM 0.1526 mL 0.7628 mL 1.5256 mL 3.8140 mL
25 mM 0.1220 mL 0.6102 mL 1.2205 mL 3.0512 mL
30 mM 0.1017 mL 0.5085 mL 1.0171 mL 2.5427 mL
40 mM 0.0763 mL 0.3814 mL 0.7628 mL 1.9070 mL
50 mM 0.0610 mL 0.3051 mL 0.6102 mL 1.5256 mL
60 mM 0.0509 mL 0.2543 mL 0.5085 mL 1.2713 mL
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ABS-752 hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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