A PROTAC
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PROTAC RAF Degrader 1

Item No. 40967

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,4R)-1-((S)-2-(2-(4-(4-(3-(2,6-difluoro-3-(propylsulfonamido)benzoyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
CAS Number
2413035-41-1
Synonyms
  • Proteolysis-targeting Chimera RAF Degrader 1
  • SJF-0628
Molecular Formula
C51H57F2N9O7S2
Formula Weight
1010.2
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C1=C(F)C(NS(=O)(CCC)=O)=CC=C1F)C2=CNC3=NC=C(C4=CC=C(N5CCN(CC5)CC(N[C@@H](C(C)(C)C)C(N6[C@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)C=C4)C=C23
InChi Code
InChI=1S/C51H57F2N9O7S2/c1-6-21-71(68,69)59-40-16-15-39(52)43(44(40)53)45(65)38-26-55-48-37(38)22-34(25-54-48)32-11-13-35(14-12-32)61-19-17-60(18-20-61)28-42(64)58-47(51(3,4)5)50(67)62-27-36(63)23-41(62)49(66)56-24-31-7-9-33(10-8-31)46-30(2)57-29-70-46/h7-16,22,25-26,29,36,41,47,59,63H,6,17-21,23-24,27-28H2,1-5H3,(H,54,55)(H,56,66)(H,58,64)/t36-,41+,47-/m1/s1
InChi Key
MBCAVOCJJAQHHT-FGUOTCRGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $138

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    Product Description

    PROTAC RAF degrader 1 is a proteolysis-targeting chimera (PROTAC) that contains the inhibitor of mutant V600E and wild-type B-RAF vemurafenib (PLX4032; Item No. 10618) conjugated to VHL ligand 1 (Item No. 21591).1 It selectively induces the degradation of B-RAF containing a valine-to-glutamate substitution at position 600 (B-RAFV600E) over wild-type B-RAF in SK-MEL-239 melanoma cells at 10 to 1,000 nM but non-selectively inhibits the activity of wild-type B-RAF and a panel of mutant B-RAF isoforms (IC50s = 5.8 and 1.87 nM). PROTAC RAF degrader 1 reduces cell viability of SK-MEL-28, SK-MEL-239, and SK-MEL-246 melanoma cells (EC50s = 215, 37, and 243 nM, respectively). In vivo, PROTAC RAF degrader 1 (50 mg/kg twice per day) reduces tumor growth and volume in an SK-MEL-246 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Alabi, S., Jaime-Figueroa, S., Yao, Z., et al. Mutant-selective degradation by BRAF-targeting PROTACs. Nat. Commun. 12(1), 920 (2021).