2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis
  4. SIAIS164018 hydrochloride

SIAIS164018 hydrochloride 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 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857).

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SIAIS164018 hydrochloride Chemical Structure

SIAIS164018 hydrochloride Chemical Structure

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Based on 1 publication(s) in Google Scholar

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SIAIS164018 hydrochloride Related Antibodies

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Description

SIAIS164018 hydrochloride 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 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857)[1].

In Vitro

SIAIS164018 (0-1 μM; 16 h) hydrochloride significantly inhibits SR cell proliferation[1].
SIAIS164018 (0-100 nM; 72 h) hydrochloride 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) hydrochloride induces a significant G1 cell cycle arrest in ALK-negative Calu-1 and MDA-MB-231 cells[1].
SIAIS164018 (0.01-1000 nM; 16h) hydrochloride 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.

SIAIS164018 hydrochloride Related Antibodies

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

919.79

Formula

C43H49Cl2N10O7P
Appearance

Solid

Color

Light brown to brown

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.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (81.54 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 1.0872 mL 5.4360 mL 10.8720 mL
5 mM 0.2174 mL 1.0872 mL 2.1744 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). 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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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). 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 1.0872 mL 5.4360 mL 10.8720 mL 27.1801 mL
5 mM 0.2174 mL 1.0872 mL 2.1744 mL 5.4360 mL
10 mM 0.1087 mL 0.5436 mL 1.0872 mL 2.7180 mL
15 mM 0.0725 mL 0.3624 mL 0.7248 mL 1.8120 mL
20 mM 0.0544 mL 0.2718 mL 0.5436 mL 1.3590 mL
25 mM 0.0435 mL 0.2174 mL 0.4349 mL 1.0872 mL
30 mM 0.0362 mL 0.1812 mL 0.3624 mL 0.9060 mL
40 mM 0.0272 mL 0.1359 mL 0.2718 mL 0.6795 mL
50 mM 0.0217 mL 0.1087 mL 0.2174 mL 0.5436 mL
60 mM 0.0181 mL 0.0906 mL 0.1812 mL 0.4530 mL
80 mM 0.0136 mL 0.0680 mL 0.1359 mL 0.3398 mL
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SIAIS164018 hydrochloride 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:

SIAIS164018SIAIS 164018SIAIS-164018PROTACsAnaplastic lymphoma kinase (ALK)EGFRApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Epidermal growth factor receptorErbB-1HER1AnticancerMDA-MB-231293TH1975SRcell migrationInhibitorinhibitorinhibit

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