1. Cell Cycle/DNA Damage
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  3. SY-1365

SY-1365 

製品番号: HY-128587 純度: 99.27%
取扱説明書

SY-1365 is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. SY-1365 exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. SY-1365 possesses anti-tumor activity in hematological and multiple aggressive solid tumors.

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SY-1365 構造式

SY-1365 構造式

CAS 番号 : 1816989-16-8

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 452 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 350 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 650 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 2000 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 3500 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

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製品説明

SY-1365 is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. SY-1365 exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. SY-1365 possesses anti-tumor activity in hematological and multiple aggressive solid tumors[1][2].

IC50 & Target[1]

CDK7

 

体外実験

SY-1365 exhibits inhibition for CDK7/CycH/MAT1 with an IC50 of 20 nM[2].
SY-1365 is a highly selective covalent CDK7 inhibitor, induces apoptosis in leukemia cells, but not in non-malignant cells[2].
SY-1365 exhibits activity in breast, ovarian, colorectal and lung cancer cells that exhibited low nM EC50 and rapid induction of apoptosis[2].

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

体内実験

SY-1365 (20mg/kg; i.v.; biw; for 35 days) inhibits tumor growth in TNBC in vivo models[2].
SY-1365 induces unique transcriptional signature[2].

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

Animal Model: Mice, HCC70 xenograft model[2]
Dosage: 20 mg/kg
Administration: Intravenous injection, twice weekly, for 35 days
Result: Inhibited tumor volume in vivo.
臨床実験
分子量

587.12

分子式

C₃₁H₃₅ClN₈O₂

CAS 番号

1816989-16-8

SMILES

O=C(C1=NC=C(NC(/C=C/CN(C)C)=O)C=C1)N[[email protected]@]2(C)CCC[[email protected]@H](NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)C2

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 : 125 mg/mL (212.90 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7032 mL 8.5161 mL 17.0323 mL
5 mM 0.3406 mL 1.7032 mL 3.4065 mL
10 mM 0.1703 mL 0.8516 mL 1.7032 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: ≥ 2.08 mg/mL (3.54 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
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Keywords:

SY-1365SY1365SY 1365CDKCyclin dependent kinasetriple negative breast cancerTNBCsmallcelllungcancerssolidtumorsCDK7/CycH/MAT1Inhibitorinhibitorinhibit

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製品名:
SY-1365
製品番号:
HY-128587
数量:
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