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  3. LXH254

LXH254 

Cat. No.: HY-112089 Purity: 99.94%
Handling Instructions

LXH254 is a potent CRAF inhibitor extracted from patent WO2018051306A1, Compound A. LXH254 also is a potent BRAF inhibitor.

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

LXH254 Chemical Structure

LXH254 Chemical Structure

CAS No. : 1800398-38-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 276 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 390 In-stock
Estimated Time of Arrival: December 31
25 mg USD 680 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

LXH254 is a potent CRAF inhibitor extracted from patent WO2018051306A1, Compound A. LXH254 also is a potent BRAF inhibitor.

IC50 & Target[1]

Braf

 

c-Raf

 

In Vitro

LXH254 (Compound A) is an adenosine triphosphate (ATP)-competitive inhibitor of BRAF (also referred to herein as b-RAF or b-Raf) and CRAF (also referred to herein as c-RAF or c- Raf) protein kinases. Throughout the present disclosure, LXH254 is also referred to as a c-RAF (or CRAF) inhibitor or a C-RAF/c-Raf kinase inhibitor. In cell-based assays, LXH254 has demonstrated anti-proliferative activity in cell lines that contain a variety of mutations that activate MAPK signaling. Moreover, LXH254 is a Type 2 ATP -competitive inhibitor of both B-Raf and C-Raf that keeps the kinase pocket in an inactive conformation, thereby reducing the paradoxical activation seen with many B-Raf inhibitors, and blocking mutant RAS-driven signaling and cell proliferation[1].

In Vivo

Treatment with LXH254 (Compound A) generates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C). LXH254 exhibits efficacy in numerous MAPK-driven human cancer cell lines and in xenograft tumors representing model tumors harboring human lesions in KRAS, NRAS and BRAF oncogenes[1].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (165.77 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9901 mL 9.9504 mL 19.9009 mL
5 mM 0.3980 mL 1.9901 mL 3.9802 mL
10 mM 0.1990 mL 0.9950 mL 1.9901 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
SCID beige female tumor-bearing NCI-H358 mice, n=8 per group, are randomized into 3 groups 14 days post tumor cell inoculation with an average tumor volume range of 259.44- 262.47mm3. Animals are administered an oral dose of either vehicle, LXH254 at 30mg/kg or 200mg/kg daily for 14 consecutive days at a dosing volume of 10 mL/kg of animal body weight during course of treatment. Tumor volumes are measured by digital caliper 3 times a week and body weights of all animals are recorded through the course of treatment.
Female nude tumor bearing Calu6 mice, n=6 per group are randomized into treatment groups on day 17 following tumor implantation, when the average tumor volume is 180 mm3. Treatments with LXH254 are initiated on Day 17 and continued for 16 days. Dosing volume is 10 mL/kg. Tumor volumes are collected at the time of randomization and twice weekly thereafter for the study duration.
Nude female mice tumor bearing NCI-H358, n=8 per group, are randomized into 2 groups with an average tumor volume range of 275.74 mm3. Animals are administered an oral dose of either vehicle or LXH254 at 100 mg/kg daily for 14 consecutive days at a dosing volume of 10 mL/kg of animal body weight during course of treatment. Tumor volumes are measured by digital caliper 3 times a week and body weights of all animals are recorded through the course of treatment[1].

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

References
Molecular Weight

502.49

Formula

C₂₅H₂₅F₃N₄O₄

CAS No.

1800398-38-2

SMILES

CC1=CC=C(NC(C2=CC(C(F)(F)F)=NC=C2)=O)C=C1C3=CC(N4CCOCC4)=NC(OCCO)=C3

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.94%

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Product Name:
LXH254
Cat. No.:
HY-112089
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LXH254

Cat. No.: HY-112089