Cart summary

You have no items in your shopping cart.

Calderasib

SKU: orb2565779

Description

Calderasib (MK-1084) is a potent and selective KRAS G12C inhibitor (IC50 = 1.2 nM) for research into KRAS-driven cancers. It demonstrates antitumor efficacy in both cellular and animal models and is being investigated as a single agent or combined with immune checkpoint inhibitors like pembrolizumab.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

Key Properties

CAS Number2641216-67-1
MW637.08
Purity98.69%
FormulaC32H31ClF2N6O4
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
TargetRas,Kras
SolubilityDMSO:80 mg/mL (125.57 mM)

Bioactivity

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.
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

MK1084, MK-1084
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Key Properties

No computed properties available.

Documents Download

Datasheet
Product Information
Download

Request a Document

Protocol Information

Calderasib (orb2565779)

  • Star
  • Star
  • Star
  • Star
  • Star
  • 0.0
Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

Login to Submit a Review

No reviews yet

Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

Step 2: Enter the in vivo formulation

(This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 12,870.00
5 mg
¥ 31,200.00
10 mg
¥ 46,670.00
25 mg
¥ 88,660.00
DispatchUsually dispatched within 5-10 working days
Bulk Enquiry