A pan-mutant B-RAF inhibitor
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Claturafenib

Item No. 46300

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-chloro-3-[(5-chloro-3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-fluorophenyl]-3-fluoro-1-azetidinesulfonamide
CAS Number
2754408-94-9
Synonyms
  • ARRY-440
  • PF-07799933
Molecular Formula
C18H15Cl2F2N5O3S
Formula Weight
490.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1C2=C(C=CC(NC3=C(Cl)C(NS(=O)(N4CC(C4)F)=O)=CC=C3F)=C2Cl)N=CN1C
InChi Code
InChI=1S/C18H15Cl2F2N5O3S/c1-26-8-23-11-4-5-12(15(19)14(11)18(26)28)24-17-10(22)2-3-13(16(17)20)25-31(29,30)27-6-9(21)7-27/h2-5,8-9,24-25H,6-7H2,1H3
InChi Key
SHENFUUACGRLOZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    Claturafenib is a pan-mutant B-RAF inhibitor.1 It inhibits heterodimer formation between C-RAF and B-RAF in melanoma cells expressing the B-RAFV600E activating mutation or the p61-B-RAFV600E splice variant but not wild-type B-RAF. Claturafenib reduces phosphorylated ERK levels in cell lines harboring various B-RAF mutations (IC50s = 0.7-179 nM) and decreases tumor volume in multiple mouse xenograft models of mutant B-RAF-expressing cancers.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yaeger, R., McKean, M.A., Haq, R., et al. A next-generation BRAF inhibitor overcomes resistance to BRAF inhibition in patients with BRAF-mutant cancers using pharmacokinetics-informed dose escalation. Cancer Discov. 14(9), 1599-1611 (2024).