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Cat. No.: HY-189666

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KRAS-IN-65

KRAS-IN-65 is an orally active KRAS inhibitor. KRAS-IN-65 inhibits KRAS G12D/G12V signaling with IC₅₀ values of 20 nM and 5 nM, respectively. KRAS-IN-65 exhibits reduced glucuronidation and intestinal stability. KRAS-IN-65 produces limited tumor growth inhibition in xenograft models. KRAS-IN-65 can be used for cancer-related research, such as non-small cell lung cancer and colorectal cancer.

For research use only. We do not sell to patients.

CAS No.: 3101978-77-9
Formula: C₃₂H₃₅ClF₂N₈O₃
Molecular Weight:653.12

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

KRAS-IN-65 Chemical Structure

CAS No.: 3101978-77-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

KRas G12D

KRas G12V

All Ras Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
SW1990	IC50	27 nM	Inhibition of pERK in SW1990 cells by cell-based pERK assay. Inhibition of pERK in SW1990 cells by cell-based pERK assay.	42720494

In Vitro

KRAS-IN-65 (compound 21) is a potent GDP-bound KRAS^G12D and KRAS^G12V inhibitor (IC₅₀ <0.2 nM), with IC₅₀ values of 20 nM and 5 nM against GMPPNP-bound KRAS, respectively; it inhibits pERK in RKN and SW1990 cells with IC₅₀ values of 76 nM and 27 nM, respectively^[1].
KRAS-IN-65 showed moderate permeability in LE-MDCK cells (21.6 × 10^-6 cm/s)^[1].
KRAS-IN-65 exhibits high intrinsic clearance in human and mouse liver microsomes (272 and 474 μL/min/mg, respectively)^[1].
KRAS-IN-65 is stable to glucuronidation in rat intestinal S9 (CL_int <6 μL/min/mg in the presence of UDPGA), and no detectable glucuronide metabolite was formed in rat hepatocytes^[1].

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

Parmacokinetics

Species	Dose	Route	AUC	CL	V_dss	F
Mice^[1]	3 mg/kg	p.o.	2660 nM·h	/	/	77 %
Mice^[1]	1 mg/kg	i.v.	1160 nM·h	22 mL/min/kg	2.4 L/kg	/
Rat^[1]	2 mg/kg	p.o.	3320 nM·h	/	/	41 %
Rat^[1]	1 mg/kg	i.v.	4020 nM·h	6.3 mL/min/kg	1.34 L/kg	/

In Vivo

Anti-cancer

KRAS-IN-65 (compound 21) (10 mg/kg; p.o.; 4 days) produced limited tumor growth inhibition in the RKN xenograft model, with a %T/C of 56%^[1].

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

Animal Model:

C.B-17/IcrHsd-PrkdcscidLystbg-J (female, RKN 10 × 10⁶/mouse)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; 4 days
Result:

In the 4-day RKN xenograft model, KRAS-IN-65 (compound 21) at 10 mg/kg p.o. showed limited tumor growth inhibition, with a %T/C of 56%.

Related Protocols :

Chemical Information

CAS No. 3101978-77-9
Molecular Weight 653.12
Formula C₃₂H₃₅ClF₂N₈O₃
SMILES

C[C@@]12CCCN(C3=NC(OC[C@@]45CCCN4C[C@@H](C5)F)=NC6=C3C=NC(C7=C(C(Cl)=CC8=C7C=NN8)CCCOC(N2)=O)=C6F)C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Phillips DP, et al. Lead Optimization of Multimutant KRAS Switch-II Pocket Macrocyclic Inhibitors via Isosteric Replacement to Improve ADME and Oral Exposure. Journal of medicinal chemistry. 2026 Sep 10;69(17):20698-20718.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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