2. Apoptosis
  3. c-Myc
  4. MYC degrader 1

MYC degrader 1 (compound A80.2HCl) is an orally available MYC degrader with antitumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC over-expressing cancer cells to CDK4/6 inhibitors.

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

MYC degrader 1 Chemical Structure

MYC degrader 1 Chemical Structure

CAS No. : 2946670-96-6

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1 mg USD 184 In-stock
5 mg USD 460 In-stock
10 mg USD 750 In-stock
25 mg USD 1500 In-stock
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Based on 1 publication(s) in Google Scholar

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MYC degrader 1 Related Antibodies

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Description

MYC degrader 1 (compound A80.2HCl) is an orally available MYC degrader with antitumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC over-expressing cancer cells to CDK4/6 inhibitors[1].

In Vitro

MYC degrader 1 (0-1000 nM; 24 h) degrades MYC in T24, C4-2, MDA-MB-231, 22RV1,T47D and UMUC14 cell lines[1].
MYC degrader 1 (10 nM; 24 h) treatment of T24 and UMUC14 cells significantly reduces the IC50 of Palbociclib (HY-50767) from 8.37 and 97.39 to 3.11 and 10.23 μM, respectively[1].
MYC degrader 1 (10 nM; 24 h) enhances the inhibition of cell cycle genes and colony formation by Palbociclib (HY-50767) in drug-resistant cancer cell lines T24, C4-2 MDA-MB-231[1].

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

MYC degrader 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: T24, C4-2, MDA-MB-231, 22RV1, T47D and UMUC14 cell lines
Concentration: 0, 10, 25, 50, 100, 500 and 1000 nM
Incubation Time: 24 h
Result: Reduced KLHL42 levels and increased RB1 levels.
In Vivo

MYC degrader 1 (6 mg/kg; p.o.; once daily for 7 days) inhibits the growth of T24 and UMUC14 xenograft tumors in mice, but had little effect on MYC-deficient xenograft tumors[1].
MYC degrader 1 (6 mg/kg; i.g.; once daily for 30 days) enhances the inhibitory effect of Palbociclib (HY-50767) on tumor growth in T24 xenograft mice[1].

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

626.07

Formula

C32H31ClF3N5O3
CAS No.
Appearance

Solid

SMILES

ClC1=CC(C2=CC(C(F)(F)F)=C(N3CCC(CNCC4=CC(CN(C5C(NC(CC5)=O)=O)C6=O)=C6C=C4)CC3)N=C2)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (159.73 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 1.5973 mL 7.9863 mL 15.9727 mL
5 mM 0.3195 mL 1.5973 mL 3.1945 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 and light). 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)

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
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 and light). 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 1.5973 mL 7.9863 mL 15.9727 mL 39.9316 mL
5 mM 0.3195 mL 1.5973 mL 3.1945 mL 7.9863 mL
10 mM 0.1597 mL 0.7986 mL 1.5973 mL 3.9932 mL
15 mM 0.1065 mL 0.5324 mL 1.0648 mL 2.6621 mL
20 mM 0.0799 mL 0.3993 mL 0.7986 mL 1.9966 mL
25 mM 0.0639 mL 0.3195 mL 0.6389 mL 1.5973 mL
30 mM 0.0532 mL 0.2662 mL 0.5324 mL 1.3311 mL
40 mM 0.0399 mL 0.1997 mL 0.3993 mL 0.9983 mL
50 mM 0.0319 mL 0.1597 mL 0.3195 mL 0.7986 mL
60 mM 0.0266 mL 0.1331 mL 0.2662 mL 0.6655 mL
80 mM 0.0200 mL 0.0998 mL 0.1997 mL 0.4991 mL
100 mM 0.0160 mL 0.0799 mL 0.1597 mL 0.3993 mL
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MYC degrader 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:

MYC degrader 12946670-96-6MYC degrader1MYC degrader-1c-MycMycMYCDegraderpRB1AntitumorInhibitorinhibitorinhibit

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