2. PROTAC Protein Tyrosine Kinase/RTK
  3. Bcr-Abl PROTACs
  4. SIAIS100 TFA

SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 TFA can be used to research chronic myeloid leukemia (CML).

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

SIAIS100 TFA Chemical Structure

SIAIS100 TFA Chemical Structure

Size Price Stock Quantity
1 mg USD 480 In-stock
5 mg USD 1250 In-stock
10 mg USD 2000 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Other Forms of SIAIS100 TFA:

SIAIS100 TFA Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 TFA can be used to research chronic myeloid leukemia (CML)[1].

In Vitro

SIAIS100 exhibits anti-proliferative activity against K562 cells with an IC50 value of 12 nM[1].
SIAIS100 degrades BCR-ABL with degradation ratio of 81.78% and 91.20% at 5 nM and 100 nM, respectively[1].
SIAIS100 (100 nM; 8 h) significantly decreases BCR-ABL in K562 cells[1].
SIAIS100 (100 nM; 6 h) induced sustained and robust BCR-ABL degradation and maintained a durable cellular response after drug removal[1].
SIAIS100 (1-1000 nM) significantly degrade mutation G250E/T315I dose-dependently accompanied by the inhibition of BCR-ABL signaling assessed by the level of p-BCR-ABL in 32D cells[1].

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

SIAIS100 TFA Related Antibodies
Molecular Weight

1004.46

Formula

C46H51ClF5N9O7S
Appearance

Solid

Color

White to off-white

SMILES

O=C1CCC(C(N1)=O)N2CC3=C(C2=O)C=CC=C3SCCCCCCN4CCN(CC4)C5CCN(CC5)C6=NC=C(C=C6C7=CC=NN7)C(NC8=CC=C(C=C8)OC(F)(Cl)F)=O.OC(C(F)(F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (99.56 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 0.9956 mL 4.9778 mL 9.9556 mL
5 mM 0.1991 mL 0.9956 mL 1.9911 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 (stored under nitrogen, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 (stored under nitrogen, 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 0.9956 mL 4.9778 mL 9.9556 mL 24.8890 mL
5 mM 0.1991 mL 0.9956 mL 1.9911 mL 4.9778 mL
10 mM 0.0996 mL 0.4978 mL 0.9956 mL 2.4889 mL
15 mM 0.0664 mL 0.3319 mL 0.6637 mL 1.6593 mL
20 mM 0.0498 mL 0.2489 mL 0.4978 mL 1.2444 mL
25 mM 0.0398 mL 0.1991 mL 0.3982 mL 0.9956 mL
30 mM 0.0332 mL 0.1659 mL 0.3319 mL 0.8296 mL
40 mM 0.0249 mL 0.1244 mL 0.2489 mL 0.6222 mL
50 mM 0.0199 mL 0.0996 mL 0.1991 mL 0.4978 mL
60 mM 0.0166 mL 0.0830 mL 0.1659 mL 0.4148 mL
80 mM 0.0124 mL 0.0622 mL 0.1244 mL 0.3111 mL
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SIAIS100 TFA 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:

SIAIS100SIAIS 100SIAIS-100Bcr-AblPROTACsAnti-cancerCMLchronic myeloid leukemiaInhibitorinhibitorinhibit

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