1. MAPK/ERK Pathway
  2. Raf

CEP-32496 (Synonyms: RXDX-105; Agerafenib)

Cat. No.: HY-15200 Purity: 99.20%
Data Sheet SDS Handling Instructions

CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2.

For research use only. We do not sell to patients.
CEP-32496 Chemical Structure

CEP-32496 Chemical Structure

CAS No. : 1188910-76-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $228 In-stock
5 mg $200 In-stock
10 mg $350 In-stock
50 mg $900 In-stock
100 mg $1200 In-stock
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Other Forms of CEP-32496:

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  • References

Description

CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. IC50 value: 14 nM/36 nM(Kd,BRAF(V600E/WT) ); 39 nM (Kd,C-Raf) Target: B-Raf/C-Raf CEP-32496 is a potent BRAF inhibitor in an in vitro binding assay for mutated BRAF(V600E) (K(d) BRAF(V600E) = 14 nM) and in a mitogen-activated protein (MAP)/extracellular signal-regulated (ER) kinase (MEK) phosphorylation (pMEK) inhibition assay in human melanoma (A375) and colorectal cancer (Colo-205) cell lines (IC(50) = 78 and 60 nmol/L). In vitro, CEP-32496 has multikinase binding activity at other cancer targets of interest; however, it exhibits selective cellular cytotoxicity for BRAF(V600E) versus wild-type cells.

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01877811 Ignyta, Inc. Solid Tumors June 2013 Phase 1
NCT03052569 Ignyta, Inc. Cancers With RET Alterations
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References
Molecular Weight

517.46

Formula

C₂₄H₂₂F₃N₅O₅

CAS No.

1188910-76-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
CEP-32496
Cat. No.:
HY-15200
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