2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRA-533

KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.

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KRA-533

KRA-533 構造式

CAS 番号 : 10161-87-2

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>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 71 在庫あり
Solution
10 mM * 1 mL in DMSO USD 71 在庫あり
Solid
5 mg $65 在庫あり
10 mg $110 在庫あり
25 mg $230 在庫あり
50 mg $394 在庫あり
100 mg $670 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

KRA-533 関連抗体

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製品説明

KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.

IC50 & Target

KRAS[1]
体外実験

KRA-533 (10 μM; 48 hours; HCC827 cells) enhances KRAS activity to a greater extent[1].
? KRA-533 (0~15 μM; 48 hours; H157 cells) enhances KRAS activity in a dose-dependent manner, which is associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death[1].
? KRA-533 (10 μM; 10 days; H292 cells) mediates cell growth suppression than those without KRAS mutation. KRA-533 (5~15 μM) can directly bind to WT, G12C, G12D and G13D mutant KRAS proteins. KRA-533 activates WT KRAS to increase its activity in a dose-dependent manner. KRA-533 further enhances the activities of active KRAS mutants[1].

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

KRA-533 関連抗体

Western Blot Analysis[1]

Cell Line: HCC827 cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: Enhanced KRAS activity to a greater extent.

Apoptosis Analysis[1]

Cell Line: H157 cells
Concentration: 0~15 μM
Incubation Time: 48 hours
Result: Enhanced KRAS activity in a dose-dependent manner, which was associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death.
体内実験

KRA-533 (0~30 mg/kg; i.p.; 28 days) suppresses tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induces apoptosis and autophagy in tumor tissues in a dose-dependent manner[1].
? KRA-533 shows optimal therapeutic index between 7.5 mg/kg and 30 mg/kg doses[1].

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

Animal Model: Nu/Nu nude mice (mutant KRAS xenografts)[1]
Dosage: 0~30 mg/kg
Administration: i.p.; 28 days
Result: Suppressed tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induced apoptosis and autophagy in tumor tissues in a dose-dependent manner.
分子量

314.18

分子式

C13H16BrNO3
CAS 番号
Appearance

Solid

Color

Off-white to light brown

SMILES

O=C(O)C1=CC=C(CCCCNC(CBr)=O)C=C1
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 : 250 mg/mL (795.72 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 3.1829 mL 15.9144 mL 31.8289 mL
5 mM 0.6366 mL 3.1829 mL 6.3658 mL
10 mM 0.3183 mL 1.5914 mL 3.1829 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.

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一般には略語で表示されます：C1V1 = C2V2

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純度とドキュメンテーション

純度: 98.73%

COA (242 KB) HNMR (268 KB) LCMS (101 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 3.1829 mL 15.9144 mL 31.8289 mL 79.5722 mL
5 mM 0.6366 mL 3.1829 mL 6.3658 mL 15.9144 mL
10 mM 0.3183 mL 1.5914 mL 3.1829 mL 7.9572 mL
15 mM 0.2122 mL 1.0610 mL 2.1219 mL 5.3048 mL
20 mM 0.1591 mL 0.7957 mL 1.5914 mL 3.9786 mL
25 mM 0.1273 mL 0.6366 mL 1.2732 mL 3.1829 mL
30 mM 0.1061 mL 0.5305 mL 1.0610 mL 2.6524 mL
40 mM 0.0796 mL 0.3979 mL 0.7957 mL 1.9893 mL
50 mM 0.0637 mL 0.3183 mL 0.6366 mL 1.5914 mL
60 mM 0.0530 mL 0.2652 mL 0.5305 mL 1.3262 mL
80 mM 0.0398 mL 0.1989 mL 0.3979 mL 0.9947 mL
100 mM 0.0318 mL 0.1591 mL 0.3183 mL 0.7957 mL
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KRA-533 Related Classifications

  • Molarity Calculator

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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:

KRA-53310161-87-2KRA533KRA 533RaspotentGTP/GDPcleavageGTP-boundapoptoticautophagiccancerInhibitorinhibitorinhibit

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製品名:
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製品番号:
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