2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Bcr-Abl
  4. SIAIS178

SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.

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SIAIS178 Chemical Structure

SIAIS178 Chemical Structure

CAS No. : 2376047-73-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 528 In-stock
Solution
10 mM * 1 mL in DMSO USD 528 In-stock
Solid
1 mg USD 200 In-stock
5 mg USD 480 In-stock
10 mg USD 650 In-stock
50 mg USD 1950 In-stock
100 mg USD 2750 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

SIAIS178 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity[1].

IC50 & Target[1]

VHL

 

Bcr-Abl

24 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
K562 IC50
24 nM
Compound: 19; SIAIS178
Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay
Growth inhibition of human K562 cells incubated for 2 days by CCK8 assay
[PMID: 31539241]
In Vitro

SIAIS178 (1-100 nM; for 16 hours) significantly reduces the BCR-ABL protein levels in a concentration dependent manner. SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5[1].
SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity in BCR-ABL driven CML cell lines. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines[1].

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

SIAIS178 Related Antibodies

Western Blot Analysis[1]

Cell Line: K562 cells
Concentration: 1, 3, 10, 30, 100 nM
Incubation Time: 16 hours
Result: Significantly reduced the BCR-ABL protein levels in a concentration dependent manner.
In Vivo

SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement [1].
SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively[1].

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

Animal Model: NOD/SCID mice with termed K562-Luc[1]
Dosage: 5, 15, and 45 mg/kg
Administration: Ip; 12 days
Result: Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement.
Animal Model: Female Wistar rats[1]
Dosage: 2 mg/kg (Pharmacokinetic Analysis)
Administration: Iv or ip; 24 hours
Result: Had T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively.
Molecular Weight

1012.68

Formula

C50H62ClN11O6S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C2=NC(C)=NC(NC3=NC=C(C(NC4=C(C=CC=C4Cl)C)=O)S3)=C2)CC1)CCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@@H](O)C5)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O
Shipping

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

DMSO : 300 mg/mL (296.24 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 0.9875 mL 4.9374 mL 9.8748 mL
5 mM 0.1975 mL 0.9875 mL 1.9750 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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
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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: ≥ 7.5 mg/mL (7.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.
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).
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

Purity: 99.36%

SDS (251 KB)

COA (244 KB) HNMR (256 KB) LCMS (138 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9875 mL 4.9374 mL 9.8748 mL 24.6870 mL
5 mM 0.1975 mL 0.9875 mL 1.9750 mL 4.9374 mL
10 mM 0.0987 mL 0.4937 mL 0.9875 mL 2.4687 mL
15 mM 0.0658 mL 0.3292 mL 0.6583 mL 1.6458 mL
20 mM 0.0494 mL 0.2469 mL 0.4937 mL 1.2343 mL
25 mM 0.0395 mL 0.1975 mL 0.3950 mL 0.9875 mL
30 mM 0.0329 mL 0.1646 mL 0.3292 mL 0.8229 mL
40 mM 0.0247 mL 0.1234 mL 0.2469 mL 0.6172 mL
50 mM 0.0197 mL 0.0987 mL 0.1975 mL 0.4937 mL
60 mM 0.0165 mL 0.0823 mL 0.1646 mL 0.4114 mL
80 mM 0.0123 mL 0.0617 mL 0.1234 mL 0.3086 mL
100 mM 0.0099 mL 0.0494 mL 0.0987 mL 0.2469 mL
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SIAIS178 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:

SIAIS1782376047-73-1SIAIS 178SIAIS-178PROTACsBcr-AbldegradationrecruitVonHippel-LindauVHLE3ubiquitinligaseanticanceractivityInhibitorinhibitorinhibit

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