製品番号: HY-139920

Oritinib

(別名: SH-1028)

1 Cited Publications

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR^WT, EGFR^L858R, EGFR^L861Q, EGFR^L858R/T790M, EGFR^d746-750 and EGFR^{d746-750/T790M} kinases, with IC₅₀s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.

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。

純度: 99.59%
CAS 番号: 2035089-28-0
分子式: C₃₁H₃₇N₇O₂
分子量:539.67

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Oritinib 構造式

CAS 番号: 2035089-28-0

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

EGFR (WT)

18 nM (IC₅₀)

EGFR^L858R

0.7 nM (IC₅₀)

EGFR^L861Q

4 nM (IC₅₀)

EGFR^L858R/T790M

0.1 nM (IC₅₀)

EGFR^d746-750

1.4 nM (IC₅₀)

EGFR^{d746-750/T790M}

0.89 nM (IC₅₀)

EGFR アイソフォーム固有の製品をすべて表示 :

体外実験

Oritinib (SH-1028) binds irreversibly to EGFR kinase by targeting cysteine-797 residue in the ATP binding site via covalent bond formation^[1].
Oritinib (0.001-10 μM) potently and selectively targets mutant EGFR cell lines in vitro^[1].
Oritinib (0.1 μM) continuously inhibits the phosphorylation of EGFR in PC-9 and NCI-H1975 cells at lower concentrations or even drug-free for at least 6 h^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

A431 (EGFR^WT), H3255 (EGFR^L858R), PC-9 (EGFR^d746-750) and NCI-H1975 (EGFR^L858R/T790M) cells
Concentration:

0.001, 0.01, 0.1, 1, and 10 μM
Incubation Time:

72 hours
Result:

Selectively inhibited EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC₅₀s of 3.93±1.12, 9.39±0.88 and 7.63±0.18 nmol/L, respectively, which were about 198-, 83- and 102-fold more sensitive than the inhibition of wild-type EGFR in A431 cells (IC₅₀=778.89±134.74 nM).

体内実験

Oral administration of Oritinib at a daily dose of 5 mg/kg significantly inhibits proliferation of tumor cells with EGFR sensitive mutation (exon 19 del) and resistant mutation (T790 M) for consecutive 14 days, with no TKI-induced weight loss in mouse xenograft models^[1].
Oritinib shows good bioavailability, and is distributed extensively from the plasma to the tissues^[1].

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

Animal Model:

6-8 weeks old female mice bearing NCI-H1975 and A431 xenograft models ^[1]
Dosage:

2.5, 5, and 15 mg/kg
Administration:

Orally administrated once daily for consecutive 14 days
Result:

Led to a significant inhibition of tumor cell growth in both PC-9 (exon 19 del) and NCI-H1975 (L858R/T790M) xenograft models.

Animal Model:

NCI-H1975 tumor-bearing mice^[1]
Dosage:

2.5, 5, and 15 mg/kg (Pharmacokinetic Analysis)
Administration:

Oral administration for 1 day or 14 consecutive days.
Result:

The T_max is 1.5-2 h, indicating rapidly distributed into tissues, including lung tumor tissues.
The AUC_0–t values in plasma were 118, 300 and 931 ng×h/mL on Day 1, while 272, 308 and 993 ng×h/ml on Day 14, respectively.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 2035089-28-0
性状 Solid
分子量 539.67
分子式 C₃₁H₃₇N₇O₂
Color Off-white to light yellow
SMILES

O=C(NC1=CC(NC2=NC(C3=C(CCCC4)N4C5=C3C=CC=C5)=CC=N2)=C(C=C1N(CCN(C)C)C)OC)C=C
別名

SH-1028
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

J Med Chem

Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. [Abstract]

2025 Aug 28;68(16):17917-17932. PMID: 40801664

溶剤 & 溶解度

体外:

DMSO : 125 mg/mL (231.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8530 mL

9.2649 mL

18.5298 mL

5 mM

0.3706 mL

1.8530 mL

3.7060 mL

10 mM

0.1853 mL

0.9265 mL

1.8530 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)

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 (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Luwei Han, et al. SH-1028, An Irreversible Third-Generation EGFR TKI, Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer. Front Pharmacol. 2021 Apr 27;12:665253. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1.8530 mL	9.2649 mL	18.5298 mL	46.3246 mL
	5 mM	0.3706 mL	1.8530 mL	3.7060 mL	9.2649 mL
	10 mM	0.1853 mL	0.9265 mL	1.8530 mL	4.6325 mL
	15 mM	0.1235 mL	0.6177 mL	1.2353 mL	3.0883 mL
	20 mM	0.0926 mL	0.4632 mL	0.9265 mL	2.3162 mL
	25 mM	0.0741 mL	0.3706 mL	0.7412 mL	1.8530 mL
	30 mM	0.0618 mL	0.3088 mL	0.6177 mL	1.5442 mL
	40 mM	0.0463 mL	0.2316 mL	0.4632 mL	1.1581 mL
	50 mM	0.0371 mL	0.1853 mL	0.3706 mL	0.9265 mL
	60 mM	0.0309 mL	0.1544 mL	0.3088 mL	0.7721 mL
	80 mM	0.0232 mL	0.1158 mL	0.2316 mL	0.5791 mL
	100 mM	0.0185 mL	0.0926 mL	0.1853 mL	0.4632 mL

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Oritinib

1 Cited Publications

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Oritinib

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MedChemExpress（MCE）の使用を引用している文献 Oritinib

EGFR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Oritinib 関連分類

HY-139920 関連分類