2. Protein Tyrosine Kinase/RTK Neuronal Signaling
  3. VEGFR c-Met/HGFR FLT3 Trk Receptor
  4. Altiratinib

Altiratinib  (Synonyms: DCC-2701)

製品番号: HY-B0791 純度: 99.29%
COA 取扱説明書 Technical Support

Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.

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Altiratinib

Altiratinib 構造式

CAS 番号 : 1345847-93-9

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 69 在庫あり
Solution
10 mM * 1 mL in DMSO USD 69 在庫あり
Solid
5 mg $61 在庫あり
10 mg $99 在庫あり
25 mg $180 在庫あり
50 mg $275 在庫あり
100 mg $495 在庫あり
500 mg $990 在庫あり
1 g   お問い合わせ  
5 g   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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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Altiratinib 関連抗体

Top Publications Citing Use of Products

VEGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

Trk Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
TrkA TrkB TrkC Trk

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.

IC50 & Target[1]

VEGFR2

9.2 nM (IC50)

Trk1

0.85 nM (IC50)

Trk2

4.6 nM (IC50)

Trk3

0.93 nM (IC50)

MET

2.7 nM (IC50)

TIE2

8 nM (IC50)

FLT3

9.3 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
K562 IC50
0.00069 μM
Compound: 25; DCC2701
Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
[PMID: 30188734]
K562 IC50
0.69 nM
Compound: 25; DCC2701
Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
[PMID: 30188734]
KM12 IC50
0.0014 μM
Compound: 25; DCC2701
Antiproliferative activity against human KM12 cells
Antiproliferative activity against human KM12 cells
[PMID: 30188734]
SK-N-SH IC50
0.0012 μM
Compound: 25; DCC2701
Antiproliferative activity against human SK-N-SH cells
Antiproliferative activity against human SK-N-SH cells
[PMID: 30188734]
体外実験

Altiratinib also inhibits MET isoforms METD1228H, MET D1228N, METY1230C, METY1230D, METY1230H, METM1250T with IC50s of 3.6, 1.3, 1.2, 0.37, 1.5 and 6 nM, respectively. Altiratinib inhibits MET phosphorylation with IC50 values of 0.85 and 2.2 nM, respectively. In the U-87 glioblastoma cell line, MET and HGF are both expressed. Altiratinib blocks autocrine activation of MET phosphorylation in these cells (IC50=6.2 nM). Altiratinib potently inhibits cellular proliferation in MET-amplified EBC-1 and MKN-45 cells, as well as TPM3-TRKA fusion KM-12 cells. Activation of MET is known to increase the motility and invasiveness of cancer cells: Altiratinib inhibits HGF-induced A549 cell migration, with an IC50 of 13 nM. Altiratinib also inhibits FLT3-ITD mutant MV-4-11 cell proliferation with an IC50 of 12 nM[1].

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

Altiratinib 関連抗体
体内実験

A single oral dose of 30 mg/kg Altiratinib leads to >95% inhibition of MET phosphorylation for the entire 24-hour period. A single 10 mg/kg oral dose of Altiratinib exhibits complete inhibition of MET phosphorylation through 12 hours and 73% inhibition at 24 hours postdose. Altiratinib dosed at 10 mg/kg twice a day leads to a significant 90% decrease in BLI signal. Altiratinib exhibits properties amenable to oral administration and exhibits substantial blood–brain barrier penetration, an attribute of significance for eventual treatment of brain cancers and brain metastases[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

510.46

分子式

C26H21F3N4O4
CAS 番号
Appearance

Solid

Color

Light yellow to khaki

SMILES

O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC(F)=C(OC4=CC(NC(C5CC5)=O)=NC=C4)C=C3F
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 : 25 mg/mL (48.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9590 mL 9.7951 mL 19.5902 mL
5 mM 0.3918 mL 1.9590 mL 3.9180 mL
10 mM 0.1959 mL 0.9795 mL 1.9590 mL
View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献
細胞実験
[1]

Altiratinib is dispensed into assay plates. Cells are added to 96-well (EBC-1, M-NFS-60, and SK-MEL-28: 2,500 cells/well; MKN-45: 5,000 cells/well; MV-4-11: 10,000 cells/well) or 384-well plates (A375 and HCT-116: 625 cells/well; BT-474, KM-12, PC-3, and U-87-MG: 1,250 cells/well). Plates are incubated for 72 hours. Viable cells are quantified using resazurin using a plate reader with excitation at 540 nm and emission at 600 nm[1].

MedChemExpress (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
[1]

Mice: Female nude mice are inoculated subcutaneously. On days 9 to 10, when tumor volumes reached 326 mg on average, mice are randomly assigned to groups and dosed once orally with 0.4% HMPC, (n=3); Altiratinib at 30 mg/kg (n=21); or Altiratinib at 10 mg/kg (n=21). At specified time points, whole blood and tumors are collected. Pharmacokinetic analysis is performed. Tumor samples are processed in the Western blot assay methods[1].

MedChemExpress (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

Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9590 mL 9.7951 mL 19.5902 mL 48.9754 mL
5 mM 0.3918 mL 1.9590 mL 3.9180 mL 9.7951 mL
10 mM 0.1959 mL 0.9795 mL 1.9590 mL 4.8975 mL
15 mM 0.1306 mL 0.6530 mL 1.3060 mL 3.2650 mL
20 mM 0.0980 mL 0.4898 mL 0.9795 mL 2.4488 mL
25 mM 0.0784 mL 0.3918 mL 0.7836 mL 1.9590 mL
30 mM 0.0653 mL 0.3265 mL 0.6530 mL 1.6325 mL
40 mM 0.0490 mL 0.2449 mL 0.4898 mL 1.2244 mL
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Altiratinib Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Altiratinib1345847-93-9DCC-2701DCC2701DCC 2701VEGFRc-Met/HGFRFLT3Trk ReceptorVascular endothelial growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Tropomyosin related kinase receptorInhibitorinhibitorinhibit

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