2. MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. Raf PERK
  4. Claturafenib

Claturafenib  (Synonyms: PF-07799933; ARRY-440)

製品番号: HY-159795 純度: 99.95%
COA 取扱説明書 Technical Support

Claturafenib ( PF-07799933) is an orally active inhibitor of pan-mutant BRAF. Claturafenib inhibits pERK in cells (IC50 value of 1.6 nM in HT29 cells). Claturafenib has anticancer activity against BRAFG469A mutant NSCLC and BRAFK601E mutant melanoma.

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Claturafenib

Claturafenib 構造式

CAS 番号 : 2754408-94-9

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 205 在庫あり
Solution
10 mM * 1 mL in DMSO USD 205 在庫あり
Solid
5 mg $190 在庫あり
10 mg $305 在庫あり
25 mg $488 在庫あり
50 mg $685 在庫あり
100 mg $960 在庫あり
1 g $2950 在庫あり
5 g   お問い合わせ  
10 g   お問い合わせ  

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Claturafenib 関連抗体

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製品説明

Claturafenib ( PF-07799933) is an orally active inhibitor of pan-mutant BRAF. Claturafenib inhibits pERK in cells (IC50 value of 1.6 nM in HT29 cells). Claturafenib has anticancer activity against BRAFG469A mutant NSCLC and BRAFK601E mutant melanoma[1].

体外実験

Claturafenib demonstrates broad inhibition of pERK levels in cell lines harboring Class I (IC50 = 0.7-7 nM), II (10-14 nmol/L), III (0.8-7.8 nM), and indel (113-179 nM) mutants, acquired BRAF p61 splice variant (59 nM), and acquired NRASQ61K (16 nM)[1].

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

Claturafenib 関連抗体
体内実験

Claturafenib (30 mg/kg; p.o.; once daily) causes tumor regressions in subcutaneous xenografts of CTG-1441 PDX, CTG-0362 PDX, and BxPC-3 in female Foxn1nu mice[1].

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

490.31

分子式

C18H15Cl2F2N5O3S
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=C1C2=C(C=CC(NC3=C(Cl)C(NS(=O)(N4CC(C4)F)=O)=CC=C3F)=C2Cl)N=CN1C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (203.95 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 2.0395 mL 10.1976 mL 20.3953 mL
5 mM 0.4079 mL 2.0395 mL 4.0791 mL
10 mM 0.2040 mL 1.0198 mL 2.0395 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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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 (5.10 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.10 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

純度: 99.95%

COA (248 KB) HNMR (290 KB) LCMS (95 KB)

取扱説明書 (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0395 mL 10.1976 mL 20.3953 mL 50.9882 mL
5 mM 0.4079 mL 2.0395 mL 4.0791 mL 10.1976 mL
10 mM 0.2040 mL 1.0198 mL 2.0395 mL 5.0988 mL
15 mM 0.1360 mL 0.6798 mL 1.3597 mL 3.3992 mL
20 mM 0.1020 mL 0.5099 mL 1.0198 mL 2.5494 mL
25 mM 0.0816 mL 0.4079 mL 0.8158 mL 2.0395 mL
30 mM 0.0680 mL 0.3399 mL 0.6798 mL 1.6996 mL
40 mM 0.0510 mL 0.2549 mL 0.5099 mL 1.2747 mL
50 mM 0.0408 mL 0.2040 mL 0.4079 mL 1.0198 mL
60 mM 0.0340 mL 0.1700 mL 0.3399 mL 0.8498 mL
80 mM 0.0255 mL 0.1275 mL 0.2549 mL 0.6374 mL
100 mM 0.0204 mL 0.1020 mL 0.2040 mL 0.5099 mL
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Claturafenib 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:

Claturafenib2754408-94-9PF-07799933 ARRY-440PF07799933PF 07799933ARRY440ARRY 440ARRY-440RafPERKRaf kinasesProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasepan-mutant BRAFHT29 cell;Inhibitorinhibitorinhibit

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