2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. Calderasib

Calderasib  (Synonyms: MK-1084)

製品番号: HY-162431 純度: 99.82%
COA 取扱説明書 Technical Support

Calderasib (MK-1084) is a selective KRAS G12C inhibitor. Calderasib exhibits anticancer activity and can be used either alone or in combination with Pembrolizumab (HY-P9902) for cancer research.

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Calderasib

Calderasib 構造式

CAS 番号 : 2641216-67-1

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 3994 在庫あり
Solution
10 mM * 1 mL in DMSO USD 3994 在庫あり
Solid
500 μg $715 在庫あり
1 mg $1140 在庫あり
5 mg $2850 在庫あり
10 mg $4280 在庫あり
25 mg $8200 在庫あり
50 mg $12300 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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Calderasib 関連抗体

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製品説明

Calderasib (MK-1084) is a selective KRAS G12C inhibitor. Calderasib exhibits anticancer activity and can be used either alone or in combination with Pembrolizumab (HY-P9902) for cancer research[1].

体外実験

Calderasib (MK-1084) (0.01-10 μM, 2 h) inhibits the SOS-catalyzed nucleotide exchange with IC50 of 1.2 nM, inhibits the phosphorylation of ERK1/2 in cell H358 with IC50 of 9 nM[2].

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

Calderasib 関連抗体
体内実験

Calderasib (MK-1084) (10-30 mg/kg, po for 14 days) exhibits antitumor efficacy in mouse MiaPaCa-2 xenograft models[2].
Calderasib (MK-1084) exhibits a good pharmacokinetic characteristics with a plasma clearance of 22 mL/min/kg, a mean residence time MRT of 1.1 h and an oral bioavailability of 61%[2].

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

Animal Model: Mouse MiaPaCa-2 xenograft models[2]
Dosage: 10-30 mg/kg
Administration: po for 14 days
Result: Inhibited tumor growth.
臨床実験
分子量

637.08

分子式

C32H31ClF2N6O4
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

FC1=C2C(OCCOC3=CC=NC(C(C)C)=C3N4C5=NC2=C(Cl)C=C5C(N6[C@@H](C)CN(C(C=C)=O)[C@H](C)C6)=NC4=O)=C(F)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (156.97 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 1.5697 mL 7.8483 mL 15.6966 mL
5 mM 0.3139 mL 1.5697 mL 3.1393 mL
10 mM 0.1570 mL 0.7848 mL 1.5697 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 (stored under nitrogen). 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
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 (stored under nitrogen). 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 1.5697 mL 7.8483 mL 15.6966 mL 39.2415 mL
5 mM 0.3139 mL 1.5697 mL 3.1393 mL 7.8483 mL
10 mM 0.1570 mL 0.7848 mL 1.5697 mL 3.9242 mL
15 mM 0.1046 mL 0.5232 mL 1.0464 mL 2.6161 mL
20 mM 0.0785 mL 0.3924 mL 0.7848 mL 1.9621 mL
25 mM 0.0628 mL 0.3139 mL 0.6279 mL 1.5697 mL
30 mM 0.0523 mL 0.2616 mL 0.5232 mL 1.3081 mL
40 mM 0.0392 mL 0.1962 mL 0.3924 mL 0.9810 mL
50 mM 0.0314 mL 0.1570 mL 0.3139 mL 0.7848 mL
60 mM 0.0262 mL 0.1308 mL 0.2616 mL 0.6540 mL
80 mM 0.0196 mL 0.0981 mL 0.1962 mL 0.4905 mL
100 mM 0.0157 mL 0.0785 mL 0.1570 mL 0.3924 mL
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Calderasib 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:

Calderasib2641216-67-1MK-1084MK1084MK 1084Rasorally activeselectiveMiaPaCa-2H358Inhibitorinhibitorinhibit

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