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製品番号: HY-171825

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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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2570251-63-5
分子式: C₄₈H₅₁N₇O₄
分子量:789.96

保管条件:

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

Data Sheet (268 KB)

SIAIS001 構造式

CAS 番号: 2570251-63-5

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- Parmacokinetics
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
Bioz

生物活性

製品説明

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

PROTACs アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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 %

化学情報

CAS 番号 2570251-63-5
分子量 789.96
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (268 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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