2. GPCR/G Protein MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. Ras PERK
  4. Opnurasib

Opnurasib  (Synonyms: JDQ-443; NVP-JDQ443)

製品番号: HY-139612 純度: 98.20% ee.: 98.02%
COA 取扱説明書 Technical Support

Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor. Opnurasib shows antitumor activity.

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Opnurasib

Opnurasib 構造式

CAS 番号 : 2653994-08-0

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 521 在庫あり
Solution
10 mM * 1 mL in DMSO USD 521 在庫あり
Solid
1 mg $132 在庫あり
5 mg $450 在庫あり
10 mg $720 在庫あり
25 mg $1400 在庫あり
50 mg $2240 在庫あり
100 mg   お問い合わせ  
200 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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Based on 7 publication(s) in Google Scholar

Other Forms of Opnurasib:

Opnurasib 関連抗体

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Ras 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
K-Ras H-Ras N-Ras Ras

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製品説明

Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor. Opnurasib shows antitumor activity[1][2].

IC50 & Target[1]

KRas G12C

 

体外実験

Opnurasib traps the GDP-bound inactive conformation of KRAS[1].
Opnurasib promotes dose-dependent reductions of phosphorylated ERK (pERK) levels and the proliferation of the KRASG12C-mutated cell lines NCI-H358 and NCI-H2122, with IC50 values of 0.018 and 0.063 μM, respectively[2].
Opnurasib covalently and selectively binds and inhibits GDP-bound KRASG12C with low reversible binding affinity to the RAS switch II pocket, and also inhibits proliferation of KRASG12C-mutated and KRAS G12C/H95, G12C/R68S, and G12C/Y96 double-mutant cell lines[2].

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

Opnurasib 関連抗体

Western Blot Analysis[2]

Cell Line: Ba/F3 cells
Concentration: 0, 0.3, 1 μM
Incubation Time: 30 min, 4 h
Result: Inhibited signaling (pERK) and proliferation of the KRAS G12C/H95 double mutants G12C/H95R and G12C/H95Q.
体内実験

Opnurasib (10-100 mg/kg, Orally, daily for 14 days) shows antitumor activity in KRAS G12C-mutated CDX models[2].
Opnurasib (Orally, 100 mg/kg, daily (JDQ443) + 7.5 mg/kg, twice daily (TNO155), for 36 days) shows greater cell growth inhibition or cell killing compared with single-agent JDQ443 when combined with TNO155[2].
Opnurasib generates categorical antitumor responses in PDX models of NSCLC and colorectal tumors that are improved by combination treatment with other agents[2].

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

Animal Model: KRAS G12C tumor-bearing nude mice (MIA PaCa-2 (PDAC); NCIH2122, LU99, HCC44, NCI-H2030 (NSCLC); and KYSE410 (esophageal cancer))[2]
Dosage: 10, 30, 100 mg/kg
Administration: Orally, daily for 14 days
Result: Inhibited the growth of all models in a dose-dependent manner.
Animal Model: Three KRAS G12C-mutated CDX models (LU99, NCI-H2030, and KYSE410)[2]
Dosage: 100 mg/kg (JDQ443) + 7.5 mg/kg (TNO155)
Administration: Orally, daily (JDQ443) or twice daily (TNO155), for 36 days
Result: Combined with TNO155, showed either greater tumor efficacy compared with each agent alone (H2030, KYSE410) or a delayed time to tumor progression (LU99).
臨床実験
分子量

526.03

分子式

C29H28ClN7O
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C=C)N1CC2(C1)CC(N3N=C(C4=CC=C5C(C=NN5C)=C4)[C@]([C@]6=C(Cl)C(C)=CC7=C6C=NN7)=C3C)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 : 80 mg/mL (152.08 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 1.9010 mL 9.5052 mL 19.0103 mL
5 mM 0.3802 mL 1.9010 mL 3.8021 mL
10 mM 0.1901 mL 0.9505 mL 1.9010 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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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

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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: ≥ 2.08 mg/mL (3.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
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: 98.20% ee.: 98.02%

COA (262 KB) HNMR (345 KB) NP-HPLC (299 KB) LCMS (103 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 1.9010 mL 9.5052 mL 19.0103 mL 47.5258 mL
5 mM 0.3802 mL 1.9010 mL 3.8021 mL 9.5052 mL
10 mM 0.1901 mL 0.9505 mL 1.9010 mL 4.7526 mL
15 mM 0.1267 mL 0.6337 mL 1.2674 mL 3.1684 mL
20 mM 0.0951 mL 0.4753 mL 0.9505 mL 2.3763 mL
25 mM 0.0760 mL 0.3802 mL 0.7604 mL 1.9010 mL
30 mM 0.0634 mL 0.3168 mL 0.6337 mL 1.5842 mL
40 mM 0.0475 mL 0.2376 mL 0.4753 mL 1.1881 mL
50 mM 0.0380 mL 0.1901 mL 0.3802 mL 0.9505 mL
60 mM 0.0317 mL 0.1584 mL 0.3168 mL 0.7921 mL
80 mM 0.0238 mL 0.1188 mL 0.2376 mL 0.5941 mL
100 mM 0.0190 mL 0.0951 mL 0.1901 mL 0.4753 mL
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Opnurasib 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:

Opnurasib2653994-08-0JDQ-443 NVP-JDQ443JDQ443JDQ 443RasPERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseNCI-H358 cellNCI-H2122 cellBa/F3 cellsAntitumor activityOrally activeNSCLCEsophageal cancerPDACInhibitorinhibitorinhibit

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