2. PROTAC Epigenetics
  3. Molecular Glues Epigenetic Reader Domain
  4. AMPTX-1

AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies.

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

AMPTX-1

AMPTX-1 Chemical Structure

CAS No. : 3033019-04-1

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AMPTX-1 Related Antibodies

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Description

AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies[1].

In Vitro

AMPTX-1 (6 h) potently degrades endogenous BRD9 in MV4-11 cells (DC50 = 0.5 nM, Dmax = 93%) and MCF-7 cells (DC50 = 2 nM, Dmax = 70%) following 6 h treatment, with a hook effect at concentrations above 100 nM[1].
AMPTX-1 (6 h) -induced BRD9 degradation in BRD9-HiBiT HEK293 cells is dependent on proteasome function, Cullin RING E3 ligase activity, and BRD9 engagement, as pre-treatment with MLN4924, Bortezomib, or BI-7273 blocks degradation[1].

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

AMPTX-1 Related Antibodies
In Vivo

AMPTX-1-ent-1 (the highly active enantiomer of AMPTX-1) (50 mg/kg; p.o.; administered twice, sampled after a single dose) induces significant BRD9 degradation in tumor tissues in the MV4-11 xenograft mouse model[1].

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

691.90

Formula

C42H53N5O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#C/C(C(N1CCC2=C(C1C)C=CC=C2CN3CCN(CC34CC4)CC5=C(OC)C=C(C6=CN(C)C(C(C)=C6C)=O)C=C5OC)=O)=C\C(C)(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (144.53 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4453 mL 7.2265 mL 14.4530 mL
5 mM 0.2891 mL 1.4453 mL 2.8906 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. 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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. 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 1.4453 mL 7.2265 mL 14.4530 mL 36.1324 mL
5 mM 0.2891 mL 1.4453 mL 2.8906 mL 7.2265 mL
10 mM 0.1445 mL 0.7226 mL 1.4453 mL 3.6132 mL
15 mM 0.0964 mL 0.4818 mL 0.9635 mL 2.4088 mL
20 mM 0.0723 mL 0.3613 mL 0.7226 mL 1.8066 mL
25 mM 0.0578 mL 0.2891 mL 0.5781 mL 1.4453 mL
30 mM 0.0482 mL 0.2409 mL 0.4818 mL 1.2044 mL
40 mM 0.0361 mL 0.1807 mL 0.3613 mL 0.9033 mL
50 mM 0.0289 mL 0.1445 mL 0.2891 mL 0.7226 mL
60 mM 0.0241 mL 0.1204 mL 0.2409 mL 0.6022 mL
80 mM 0.0181 mL 0.0903 mL 0.1807 mL 0.4517 mL
100 mM 0.0145 mL 0.0723 mL 0.1445 mL 0.3613 mL
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AMPTX-1 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:

AMPTX-13033019-04-1AMPTX1AMPTX 1Molecular GluesEpigenetic Reader DomainMCF-7 cellsproteasomeMV4-11 cellsCullin RING E3 ligase pathwayBRD9-HiBiT HEK293 cellsDDB1DCAF16solid and haematological malignanciesE3 ligaseBRD9Inhibitorinhibitorinhibit

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