1. PROTAC Epigenetics
  2. PROTACs Epigenetic Reader Domain
  3. SMD-3040 TFA

SMD-3040 TFA is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 TFA can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 TFA can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))

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

SMD-3040 TFA Chemical Structure

SMD-3040 TFA Chemical Structure

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Description

SMD-3040 TFA is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 TFA can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 TFA can be used in the study of tumors such as melanoma[1]. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))

In Vitro

SMD-3040 (0-1 μM; 1-48 h) TFA can effectively degrade SMARCA2 in cells such as Hela, SK-Mel-5 and SK-Mel-28[1].
SMD-3040 (7 days) TFA significantly inhibits cell growth in SMARCA4-deficient cancer cell lines (such as SK-Mel-5, H838, A549, etc.) with GI50 of 8.8-119 nM[1].

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

Western Blot Analysis[1]

Cell Line: SK-Mel-5 and SK-Mel-28 cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300 and 1000 nM
Incubation Time: 24 h
Result: Inhibited the level of SMARCA2.
Had DC50 values of 20 and 35 nM in K-Mel-5 and SK-Mel-28 cells.
In Vivo

SMD-3040 (25-50 mg/kg; intravenous injection; twice weekly; two weeks) TFA exhibits antitumor activity in a xenograft mouse model of human melanoma[1].

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

Animal Model: Xenograft mouse models treated SK-Mel-5 melanoma cell line carrying SMARCA4 gene deletion[1]
Dosage: 25 and 50 mg/kg
Administration: Intravenous injection; twice weekly; two weeks
Result: Effectively inhibited tumor growth in two different smarca4-deficient xenograft models.
Was well-tolerated in mice.
Molecular Weight

1057.23

Formula

C54H67F3N10O7S

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N[C@H](C(N1[C@H](C(N[C@H](C2=CC=C(C3=C(C)N=CS3)C=C2)C)=O)C[C@@H](O)C1)=O)C(C)(C)C)[C@H]4CC[C@H](CN5CC6(CCC(N7N=CC(C8=C(N)N=NC(C9=C(O)C=CC=C9)=C8)=C7)CC6)C5)CC4.O=C(O)C(F)(F)F

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 (94.59 mM; Need ultrasonic and warming; 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 0.9459 mL 4.7293 mL 9.4587 mL
5 mM 0.1892 mL 0.9459 mL 1.8917 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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. 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 0.9459 mL 4.7293 mL 9.4587 mL 23.6467 mL
5 mM 0.1892 mL 0.9459 mL 1.8917 mL 4.7293 mL
10 mM 0.0946 mL 0.4729 mL 0.9459 mL 2.3647 mL
15 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5764 mL
20 mM 0.0473 mL 0.2365 mL 0.4729 mL 1.1823 mL
25 mM 0.0378 mL 0.1892 mL 0.3783 mL 0.9459 mL
30 mM 0.0315 mL 0.1576 mL 0.3153 mL 0.7882 mL
40 mM 0.0236 mL 0.1182 mL 0.2365 mL 0.5912 mL
50 mM 0.0189 mL 0.0946 mL 0.1892 mL 0.4729 mL
60 mM 0.0158 mL 0.0788 mL 0.1576 mL 0.3941 mL
80 mM 0.0118 mL 0.0591 mL 0.1182 mL 0.2956 mL
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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.

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Product Name:
SMD-3040 TFA
Cat. No.:
HY-156568A
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