SIAIS164018

Cat. No.: HY-147219: FAQs
Data Sheet Handling Instructions

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SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857).

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

SIAIS164018 Chemical Structure

CAS No. : 2353492-68-7

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Other Forms of SIAIS164018:

SIAIS164018 hydrochloride Get quote

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC₅₀: 2.5 nM (ALK), 6.6 nM (ALK G1202R)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	21 nM Compound: 6; SIAIS164018	Antiproliferative activity against human 293T cells overexpressing ALK G1202R mutant assessed as cell growth inhibition after 72 hrs Antiproliferative activity against human 293T cells overexpressing ALK G1202R mutant assessed as cell growth inhibition after 72 hrs	[PMID: 34138566]
NCI-H1975	IC₅₀	42 nM Compound: 6; SIAIS164018	Antiproliferative activity against human H1975 cells overexpressing EGFR L858R/T790M mutant assessed as cell growth inhibition after 72 hrs Antiproliferative activity against human H1975 cells overexpressing EGFR L858R/T790M mutant assessed as cell growth inhibition after 72 hrs	[PMID: 34138566]
SR	IC₅₀	2 nM Compound: 6; SIAIS164018	Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human SR cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 34138566]

In Vitro

SIAIS164018 (0-1 μM; 16 h) significantly inhibits SR cell proliferation^[1].
SIAIS164018 (0-100 nM; 72 h) shows better cell proliferation inhibition than Brigatinib does in ALK (G1202R) over-expressing 293T and EGFR expressing H1975 cell lines^[1].
SIAIS164018 (100 nM; 24 or 48 h) induces a significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells^[1].
SIAIS164018 (0.01-1000 nM; 16h) down-regulates the protein level of FAK, PYK2, FER, RSK1, and GAK in ALK-positive SR and ALK-negative Calu-1 cell lines^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	SR cells
Concentration:	0-1 μM
Incubation Time:	16 h
Result:	Significantly inhibited SR cell proliferation with an IC₅₀ value of 2 nM.

Cell Proliferation Assay^[1]

Cell Line:	ALK (G1202R) over-expressing 293T and EGFR expressing H1975 cell lines
Concentration:	0-100 nM
Incubation Time:	72 h
Result:	Exhibited better cell proliferation inhibition than Brigatinib does in ALK (G1202R) over-expressing 293T and EGFR expressing H1975 cell lines with IC₅₀s 21 and 42 nM, respectively.

Cell Cycle Analysis^[1]

Cell Line:	ALK-negative Calu-1 and MDA-MB-231 cells
Concentration:	100 nM
Incubation Time:	24 or 48 h
Result:	Induced a significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells.

Western Blot Analysis^[1]

Cell Line:	SR and Calu-1 cells
Concentration:	0.01, 0.1, 1, 10, 100 and 1000 nM
Incubation Time:	16 h
Result:	Down-regulated the protein level of FAK, PYK2, FER, RSK1, and GAK.

Molecular Weight

883.33

Formula

C₄₃H₄₈ClN₁₀O₇P

CAS No.

2353492-68-7

SMILES

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCC(N4CCN(C5CCN(CC5)C6=CC=C(C(OC)=C6)NC7=NC=C(C(NC8=C(P(C)(C)=O)C=CC=C8)=N7)Cl)CC4)=O)=CC=C3)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (113.21 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	1.1321 mL	5.6604 mL	11.3208 mL
5 mM	0.2264 mL	1.1321 mL	2.2642 mL
10 mM	0.1132 mL	0.5660 mL	1.1321 mL

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.83 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)

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

Handling Instructions (2659 KB)

References

[1]. Ren C, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. J Med Chem. 2021 Jul 8;64(13):9152-9165. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.1321 mL	5.6604 mL	11.3208 mL	28.3020 mL
	5 mM	0.2264 mL	1.1321 mL	2.2642 mL	5.6604 mL
	10 mM	0.1132 mL	0.5660 mL	1.1321 mL	2.8302 mL
	15 mM	0.0755 mL	0.3774 mL	0.7547 mL	1.8868 mL
	20 mM	0.0566 mL	0.2830 mL	0.5660 mL	1.4151 mL
	25 mM	0.0453 mL	0.2264 mL	0.4528 mL	1.1321 mL
	30 mM	0.0377 mL	0.1887 mL	0.3774 mL	0.9434 mL
	40 mM	0.0283 mL	0.1415 mL	0.2830 mL	0.7075 mL
	50 mM	0.0226 mL	0.1132 mL	0.2264 mL	0.5660 mL
	60 mM	0.0189 mL	0.0943 mL	0.1887 mL	0.4717 mL
	80 mM	0.0142 mL	0.0708 mL	0.1415 mL	0.3538 mL
	100 mM	0.0113 mL	0.0566 mL	0.1132 mL	0.2830 mL

SIAIS164018 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.

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