2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Anaplastic lymphoma kinase (ALK)
  4. SIAIS001

SIAIS001 is a CRBN-dependent ALK PROTAC degrader with a DC50 of 3.9 nM. SIAIS001 induces ALK protein degradation via the ubiquitin-proteasome system. SIAIS001 induces G1/S phase cell cycle arrest and inhibits proliferation of cancer cells. SIAIS001 can be used for the research of anaplastic large-cell lymphomas.
(Pink: Anaplastic lymphoma kinase (ALK) ligand (HY-13011); Blue: Cereblon ligand (HY-138793); Black: linker).

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

SIAIS001

SIAIS001 Chemical Structure

CAS No. : 2570251-63-5

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SIAIS001 Related Antibodies

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Description

SIAIS001 is a CRBN-dependent ALK PROTAC degrader with a DC50 of 3.9 nM. SIAIS001 induces ALK protein degradation via the ubiquitin-proteasome system. SIAIS001 induces G1/S phase cell cycle arrest and inhibits proliferation of cancer cells. SIAIS001 can be used for the research of anaplastic large-cell lymphomas[1]. (Pink: Anaplastic lymphoma kinase (ALK) ligand (HY-13011); Blue: Cereblon ligand (HY-138793); Black: linker).

IC50 & Target[1]

Cereblon

 

Cellular Effect
Cell Line Type Value Description References
SR IC50
0.9 nM
Compound: C26; SIAIS001
Antiproliferative activity against ALK positive human SR cells
Antiproliferative activity against ALK positive human SR cells
[PMID: 33751979]
In Vitro

SIAIS001 (0.05-500 nM) potently degrades ALK protein via the ubiquitin-proteasome system in SR (NPM-ALK fusion) anaplastic large-cell lymphoma cells, with a DC50 of 3.9 nM and a maximum degradation of 70.3%[1].
SIAIS001 inhibits SR (NPM-ALK fusion) cell proliferation with an IC50 of 0.9 nM[1].
SIAIS001 (0.05-500 nM) inhibits ALK downstream signaling in SR (NPM-ALK fusion) anaplastic large-cell lymphoma cells, reducing phosphorylated ALK and phosphorylated STAT3[1].
SIAIS001 potently inhibits wild-type ALK kinase activity with an IC50 of 3.3 nM and inhibits ALKG1202R mutant kinase activity with an IC50 of 94.6 nM[1].
SIAIS001 (100 nM; 24 h) promotes G1/S phase cell cycle arrest in SR (NPM-ALK fusion) anaplastic large-cell lymphoma cells[1].

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

SIAIS001 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: SR (NPM-ALK fusion) anaplastic large-cell lymphoma cells
Concentration: 100 nM
Incubation Time: 24 h
Result: Induced G1/S cell cycle arrest in SR cells.
Reduced the percentage of cells in S phase to a level significantly lower than that observed with Alectinib (HY-13011) treatment, indicating stronger G1/S arrest than Alectinib.
Parmacokinetics
Species Dose Route Cmax Bioavailability
Rat[1] 2 mg/kg i.p. 83.45 ng/mL /
Rat[1] 10 mg/kg p.o. 100 ng/mL 16 %
Molecular Weight

789.96

Formula

C48H51N7O4
CAS No.
SMILES

N#CC1=CC(NC2=C3C(C4=C(C2(C)C)C=C(N5CCC(CC5)N6CCN(CCCC#CC7=CC=CC8=C7CN(C9C(NC(CC9)=O)=O)C8=O)CC6)C(CC)=C4)=O)=C3C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SIAIS001 Related Classifications

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The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

SIAIS0012570251-63-5SIAIS 001SIAIS-001PROTACsAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALKphosphorylated STAT3SR (NPM-ALK fusion)anaplastic large-cell lymphoma cellsubiquitin-proteasome systemG1/S phase cell cycle arrestALK-G1202R mutantanaplastic large-cell lymphomasInhibitorinhibitorinhibit

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