ARV-471 (Synonyms: ARV-471) |
カタログ番号GC62723
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ARV-471は局所進行性または転移性のER+/HER2乳癌患者の治療のための、経口で生物活性のあるエストロゲン受容体標的（ER標的）PROTACである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2229711-68-4
Sample solution is provided at 25 µL, 10mM.
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ARV-471は局所進行性または転移性のER+/HER2乳癌患者の治療のための、経口で生物活性のあるエストロゲン受容体標的（ER標的）PROTACである。
ARV-471はMCF-7細胞とESR1変異株を含む野生型および変異型ER の分解を誘導する(≥90%)。ARV-471はMCF7、T47D、T47D ER-Y537SおよびT47D ER-D538G細胞の増殖を阻害し、GI50はそれぞれ3.3、4.5、7.9、5.7 nMである。
ARV-471 (10および30 mpk, 27日間)はESR1変異を有する患者由来腫瘍異種移植モデルの増殖を抑制することができ、良好な腫瘍抑制効果を有する。ARV-471 (3, 10 および30 mg/kg, 28日間)はMCF7同所性異種移植モデルにおいて用量依存的に腫瘍増殖を抑制し、ER分解を促進した(≥94%)。
References:
[1] Snyder L B, Flanagan J J, Qian Y, et al. The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC for the treatment of patients with breast cancer[J]. Cancer Res, 2021, 81(13): 44.
[2] Gough S M, Flanagan J J, Teh J, et al. Oral estrogen receptor PROTAC® vepdegestrant (ARV-471) is highly efficacious as monotherapy and in combination with CDK4/6 or PI3K/mTOR pathway inhibitors in preclinical ER+ breast cancer models[J]. Clinical Cancer Research, 2024.
| 細胞実験[1]: | |
細胞株 | MCF7、T47D、T47D ER-Y537SおよびT47D ER-D538G |
準備方法 | 細胞をARV-471で処理した5日後、ATPレベルはluminescent Cell-Titer Glo assayを用いて測定し、細胞生存率を決定する |
反応条件 | 0.1,1,10,100 and1000 nM, 5日間 |
アプリケーション | ARV-471はin-vitroでWTと変異型ER依存性乳がん細胞の増殖を阻害した |
| 動物実験 [1]: | |
動物モデル | MCF7同所性異種移植モデル |
準備方法 | マウスの腫瘍体積の平均値が200 mm3に達した時点で、ARV-471を1日1回28日間連続経口投与した |
投与形態 | 3, 10 および30 mg/kg/day, 28日間, p.o. |
アプリケーション | ARV-471は1日3, 10 および30 mg/kgの用量で用量依存的に腫瘍増殖を抑制し、腫瘍（体積）抑制率はそれぞれ85%, 98%, および120%である |
References: | |
| Cas No. | 2229711-68-4 | SDF | |
| 同義語 | ARV-471 | ||
| Formula | C45H49N5O4 | M.Wt | 723.9 |
| 溶解度 | DMSO : 110 mg/mL (151.95 mM; Need ultrasonic) | Storage | Store at -20°C, sealed storage, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3814 mL | 6.907 mL | 13.8141 mL |
| 5 mM | 276.3 μL | 1.3814 mL | 2.7628 mL |
| 10 mM | 138.1 μL | 690.7 μL | 1.3814 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)