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

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 Estructura química

No. CAS : 2641216-67-1

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
500 μg En stock
1 mg En stock
5 mg En stock
10 mg En stock
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Calderasib Related Antibodies

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Descripciòn

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].

In Vitro

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 Related Antibodies
In Vivo

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.
Ensayo clínico
Peso molecular

637.08

Fòrmula

C32H31ClF2N6O4
No. CAS
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, stored under nitrogen

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

Solvente y solubilidad
In Vitro: 

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
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.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

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(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.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación
Referencias

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

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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Nombre del producto:
Calderasib
Cat. No.:
HY-162431
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