1. Protein Tyrosine Kinase/RTK
  2. RET
  3. Pralsetinib

Pralsetinib (Synonyms: BLU-667)

製品番号: HY-112301 純度: 99.56%
取扱説明書

Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively.

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Pralsetinib 構造式

Pralsetinib 構造式

CAS 番号 : 2097132-94-8

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 153 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 65 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 130 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 185 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 685 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1080 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

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製品説明

Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively[1].

IC50 & Target

IC50: 0.4 nM (Wild type RET), 0.3 nM (RET V804L), 0.4 nM (RET V804M), 0.4 nM (RET M918T), 0.4 nM (CCDC6-RET)[1]

体外実験

Pralsetinib (BLU-667) demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants[1].
Pralsetinib (BLU-667) demonstrates potent activity (IC50=0.4 nM) against common oncogenic RET alterations, including RET M918T, an activating mutation found in MTC, as well as the CCDC6-RET fusion observed in PTC and NSCLC[1].
Pralsetinib (BLU-667) suppresses RET pathway signaling in a panel of RET-driven cell lines: LC2/ad (CCDC6-RET, NSCLC), MZ-CRC-1 (RET M918T, MTC), and TT (RET C634W, MTC)[1].

体内実験

Pralsetinib (BLU-667) potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting vascular endothelial growth factor receptor 2 (VEGFR-2)[1].
Pralsetinib (BLU-667) shows dose dependent activity against both KIF5B-RET Ba/F3 and KIF5B-RET V804L Ba/F3 allograft tumors with doses as low as 10 mg/kg twice-daily[1].

臨床実験
分子量

533.60

分子式

C₂₇H₃₂FN₉O₂

CAS 番号

2097132-94-8

SMILES

O=C([[email protected]@]1(OC)CC[[email protected]](C2=NC(NC3=NNC(C)=C3)=CC(C)=N2)CC1)N[[email protected]](C4=CC=C(N5N=CC(F)=C5)N=C4)C

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
溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (187.41 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8741 mL 9.3703 mL 18.7406 mL
5 mM 0.3748 mL 1.8741 mL 3.7481 mL
10 mM 0.1874 mL 0.9370 mL 1.8741 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[2]

KIF5B-RET Ba/F3 cells are exposed to compound concentrations ranging from 25 µM to 95.4 pM for 48 hours, and proliferation is assessed with Cell Titer Glo. TT, MZ-CRC-1, TPC-1 or LC2/ad cells are exposed to compound for 4 days and proliferation is measured by BrdU incorporation[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[2]

Mice[2]

BALB/c nude mice are inoculated subcutaneously into the right flank with KIF5B-RET Ba/F3 cells, KIF5B-RET V804L Ba/F3 cells, or TT cells. For all experiments, mice are dosed twice-daily with vehicle, 3 mg/kg, 10 mg/kg, or 30 mg/kg Pralsetinib (Blu667) or once-daily with 60 mg/kg Pralsetinib (Blu667; administered orally) or 60 mg/kg XL184[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

純度: 99.56%

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Keywords:

PralsetinibBLU-667BLU667BLU 667RETInhibitorinhibitorinhibit

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製品名:
Pralsetinib
製品番号:
HY-112301
数量:
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