1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Apoptosis
  2. EGFR
    Apoptosis
  3. Poziotinib

Poziotinib (Synonyms: HM781-36B; NOV120101)

目录号: HY-15730 纯度: 99.96%
产品使用指南

HM781-36B 是一种口服活性,不可逆的泛 HER 抑制剂。HM781-36B 抑制 EGFRwt、HER-2 和 HER-4 的 IC50 值分别为 3.2、5.3 和 23.5 nM,对突变的 EGFR,包括 EGFRT790M 和 EGFRL858R/T790MIC50 值分别为 4.2 和 2.2 nM。具有良好的抗肿瘤活性。

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Poziotinib Chemical Structure

Poziotinib Chemical Structure

CAS No. : 1092364-38-9

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1  mL in DMSO ¥1089 In-stock
5 mg ¥990 In-stock
10 mg ¥1450 In-stock
50 mg ¥5200 In-stock
100 mg ¥8000 In-stock
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Description

Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFRwt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFRT790M and EGFRL858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity[1][2].

IC50 & Target

IC50: 3.2 nM (EGFRwt), 5.3 nM (HER-2), 23.5 nM (HER-4) 4.2 nM (EGFRT790M), 2.2 nM (EGFRL858R/T790M)[2]

In Vitro

The IC50 levels of Poziotinib (HM781-36B) for N87 and SNU216 were 0.001 and 0.004 μM, respectively, which was 10-1000 fold lower than the IC50 levels of other HER family TKIs. HM781-36B more potently inhibited the phosphorylation of HER family and downstream proteins, and induced apoptosis and G1 arrest compared to ZD1839 or GW572016[1].
Poziotinib (HM781-36B) also shows excellent selectivity with other kinases with greater than 100- to 1,000- fold IC50 values compared with EGFR family members. Poziotinib (HM781-36B) possesses a functional α,β‐unsaturated carbonyl group as Michael acceptor moiety at the C6 position that allows covalent modifications of the EGFR kinase domain active site[2].
The addition of HM781-36B induced potent growth inhibition in both DiFi cells with EGFR overexpression and SNU-175 cells (IC50=0.003 and 0.005 μM, respectively). Furthermore, HM781-36B induced G1 arrest of the cell cycle and apoptosis, and reduced the levels of HER family and downstream signaling molecules, pERK and pAKT, as well as nonreceptor/cytoplasmic tyrosine kinase, BMX[3].

In Vivo

The growth of tumors in mice treated with HM781-36B alone or in combination with 5-FU was significantly inhibited compared with control mice, and tumor volume in mice receiving coadministraion of HM781-36B and 5-FU was smaller than tumor volume in mice receiving HM781-36B only[1].

Clinical Trial
Molecular Weight

491.34

Formula

C₂₃H₂₁Cl₂FN₄O₃

CAS No.

1092364-38-9

SMILES

C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C(Cl)=C4F)N=CN=C3C=C2OC)CC1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 135 mg/mL (274.76 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0353 mL 10.1763 mL 20.3525 mL
5 mM 0.4071 mL 2.0353 mL 4.0705 mL
10 mM 0.2035 mL 1.0176 mL 2.0353 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.25 mg/mL (4.58 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (4.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.25 mg/mL (4.58 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (4.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 MCE 网站选购。
References

Purity: 99.96%

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Keywords:

PoziotinibHM781-36BNOV120101NOV 120101NOV-120101EGFRApoptosisEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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