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Calderasib

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Catalog No. T86905Cas No. 2641216-67-1
Alias MK-1084, MK1084

Calderasib (MK-1084) is a selective KRAS G12C inhibitor with an IC50 value of 1.2 nM . Calderasib (MK-1084) exhibits significant anticancer activity, and it can be employed either as a monotherapy or in combination with the PD-1 inhibitor Pembrolizumab, providing a versatile approach for the investigation of KRAS-mutant driven cancers.

Calderasib

Calderasib

😃Good
Purity: 98.69%
Catalog No. T86905Alias MK-1084, MK1084Cas No. 2641216-67-1
Calderasib (MK-1084) is a selective KRAS G12C inhibitor with an IC50 value of 1.2 nM . Calderasib (MK-1084) exhibits significant anticancer activity, and it can be employed either as a monotherapy or in combination with the PD-1 inhibitor Pembrolizumab, providing a versatile approach for the investigation of KRAS-mutant driven cancers.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$943-In Stock
5 mg$2,360-In Stock
10 mg$3,550-In Stock
25 mg$6,780-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.69%
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COA LCMS HNMR

Product Introduction

Bioactivity
Description
Calderasib (MK-1084) is a selective KRAS G12C inhibitor with an IC50 value of 1.2 nM . Calderasib (MK-1084) exhibits significant anticancer activity, and it can be employed either as a monotherapy or in combination with the PD-1 inhibitor Pembrolizumab, providing a versatile approach for the investigation of KRAS-mutant driven cancers.
In vitro
Calderasib (MK-1084) (0.01-10 μM, 2 h) inhibited the phosphorylation of ERK1/2 in H358 cells with an IC50 of 9 nM. [2]
In vivo
Calderasib (MK-1084) (10-30 mg/kg, administered orally for 14 consecutive days) was given to the MiaPaCa-2 xenograft mouse model, and the Results demonstrated that Calderasib (MK-1084) significantly inhibited tumor growth.[2]
SynonymsMK-1084, MK1084
Chemical Properties
Molecular Weight637.08
FormulaC32H31ClF2N6O4
Cas No.2641216-67-1
SmilesO=C1N2C=3C(C(=N1)N4C(C)CN(C(C=C)=O)C(C)C4)=CC(Cl)=C(N3)C=5C(=C(F)C=CC5F)OCCOC=6C2=C(C(C)C)N=CC6
ColorYellow
AppearanceSolid
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 80 mg/mL (125.57 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5697 mL7.8483 mL15.6966 mL78.4831 mL
5 mM0.3139 mL1.5697 mL3.1393 mL15.6966 mL
10 mM0.1570 mL0.7848 mL1.5697 mL7.8483 mL
20 mM0.0785 mL0.3924 mL0.7848 mL3.9242 mL
50 mM0.0314 mL0.1570 mL0.3139 mL1.5697 mL
100 mM0.0157 mL0.0785 mL0.1570 mL0.7848 mL

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