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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).

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No. CAS: 2570251-63-5
Fòrmula: C₄₈H₅₁N₇O₄
Peso molecular:789.96

Almacenamiento:

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

Data Sheet (268 KB)

SIAIS001 Chemical Structure

No. CAS: 2570251-63-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Bioz

Actividad biológica

Descripciòn

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

Ver todos los productos específicos de isoformas PROTACs :

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 ALK^G1202R 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.

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	C_max	Bioavailability
Rat^[1]	2 mg/kg	i.p.	83.45 ng/mL	/
Rat^[1]	10 mg/kg	p.o.	100 ng/mL	16 %

Chemical Information

No. CAS 2570251-63-5
Peso molecular 789.96
Fòrmula C₄₈H₅₁N₇O₄
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Ren C, et al. Structure-based discovery of SIAIS001 as an oral bioavailability ALK degrader constructed from Alectinib. Eur J Med Chem. 2021;217:113335. [Content Brief]

Calculators

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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