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製品番号: HY-146022

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SIAIS117

SIAIS117 is an ALK PROTAC degrader constructed based on Brigatinib (HY-12857) and VHL-1. SIAIS117 exhibits activity not only against wild-type ALK fusion proteins, but also effectively degrades the highly drug-resistant ALK G1202R mutant fusion protein. SIAIS117 significantly inhibits the proliferation of non-small cell lung cancer, small cell lung cancer, anaplastic large cell lymphoma, and drug-resistant cells expressing EML4-ALK G1202R. SIAIS117 can be used in relevant research on the above-mentioned malignant tumors.
(Pink: Anaplastic lymphoma kinase (ALK) Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker (HY-W014125)).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 2353494-84-3
分子式: C₅₇H₇₆ClN₁₀O₇PS
分子量:1111.77

保管条件:

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

Data Sheet (269 KB)

SIAIS117 構造式

CAS 番号: 2353494-84-3

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

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

生物活性

製品説明

SIAIS117 is an ALK PROTAC degrader constructed based on Brigatinib (HY-12857) and VHL-1. SIAIS117 exhibits activity not only against wild-type ALK fusion proteins, but also effectively degrades the highly drug-resistant ALK G1202R mutant fusion protein. SIAIS117 significantly inhibits the proliferation of non-small cell lung cancer, small cell lung cancer, anaplastic large cell lymphoma, and drug-resistant cells expressing EML4-ALK G1202R. SIAIS117 can be used in relevant research on the above-mentioned malignant tumors^[1]. (Pink: Anaplastic lymphoma kinase (ALK) Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker (HY-W014125)).

IC₅₀ & Target

VHL

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
NCI-H2228	IC₅₀	46 nM Compound: 18; SIAI5117	Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 32179332]
NCI-H69	IC₅₀	799 nM Compound: 18; SIAI5117	Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell proliferation Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell proliferation	[PMID: 32179332]
SR	IC₅₀	1.7 nM Compound: 18; SIAI5117	Antiproliferative activity against human SR cells assessed as reduction in cell growth Antiproliferative activity against human SR cells assessed as reduction in cell growth	[PMID: 32179332]

体外実験

SIAIS117 (7-189 nM) effectively degrades wild-type and ALK^G1202R mutant ALK fusion proteins in SR, H2228, and 293T cells with DC₅₀ values of 7 nM, ~100 nM, and 189 nM, respectively, and does not degrade off-target Aurora A protein^[1].
SIAIS117 (1.7-166 nM) potently inhibits proliferation of SR, H2228, and ALK^G1202R mutant ALK-expressing cells with IC₅₀ values of 1.7 nM, 46 nM, and 166 nM, respectively, and inhibits growth of SCLC cell lines at concentrations where brigatinib is ineffective^[1].

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

Cell Proliferation Assay

Cell Line:

NSCLC cell line H2228, Small cell lung cancer cell lines (NCI-H69, NCI-H1688)^[1]
Concentration:

0-10 μM
Incubation Time:

72 h
Result:

Inhibited cell growth with an about two folds lower IC₅₀ value (46 nM) comparing to SIAIS117NC (114 nM). Showed a good growth inhibition effect on NCI-H69 and NCI-H1688 cell line, with IC₅₀ values of 799 and 259 nM, respectively.

Western Blot Analysis

Cell Line:

SR, H2228^[1]
Concentration:

0, 1, 10, 50, 100, 500 nM
Incubation Time:

24 h
Result:

Inhibited all of the phosphorylation of ALK at 10 nM and inhibited pSTAT3 in SR cell, degraded ALK proteins at the concentration starting from 50 nM in H2228 cell, and significantly downregulated UCK2 and GAK. Caused sustained degradation of ALK protein in SR cells.

化学情報

CAS 番号 2353494-84-3
分子量 1111.77
分子式 C₅₇H₇₆ClN₁₀O₇PS
SMILES

COC(C=C1N(CC2)CCC2NC(CCCCCCCCCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(NCC4=CC=C(C5=C(N=CS5)C)C=C4)=O)=O)=O)=O)=C(C=C1)NC6=NC=C(Cl)C(NC7=C(C=CC=C7)P(C)(C)=O)=N6
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 (269 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]. Song X, et al. Two novel strategies to overcome the resistance to ALK tyrosine kinase inhibitor drugs: Macrocyclic inhibitors and proteolysis-targeting chimeras. MedComm. 2021 Sep;2(3):341-350. [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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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