A KRAS inhibitor
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Deltarasin (hydrochloride)

Item No. 9001536

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-[(2S)-2-(2-phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole, hydrochloride
CAS Number
1440898-82-7
Molecular Formula
C40H37N5O • 2.4HCl
Formula Weight
691.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
241, 290 nm
SMILES
C12=CC=CC=C1N=C(C3=CC=CC=C3)N2[C@@H](C4CCNCC4)COC5=CC=C(C6=NC(C=CC=C7)=C7N6CC8=CC=CC=C8)C=C5.Cl.Cl
InChi Code
InChI=1S/C40H37N5O.2ClH/c1-3-11-29(12-4-1)27-44-36-17-9-7-15-34(36)42-39(44)32-19-21-33(22-20-32)46-28-38(30-23-25-41-26-24-30)45-37-18-10-8-16-35(37)43-40(45)31-13-5-2-6-14-31;;/h1-22,30,38,41H,23-28H2;2*1H/t38-;;/m1../s1
InChi Key
SZLAQKGNNWXKSN-VROLVAQFSA-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

    $304

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    Cayman Chemical
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    Product Description

    Deltarasin is a small molecule that binds to the farnesyl-binding pocket of PDEδ (Kd = 41 nM) in cells thus inhibiting its interaction with KRAS and disrupting RAS signaling.1 Treatment of human pancreatic ductal adenocarcinoma cell models with 5 μM deltarasin has been reported to prevent KRAS plasma membrane localization and subsequent solubilization by PDEδ, resulting in reduced proliferation and increased cell death of Panc-Tu-I tumor cells.1 Furthermore, in nude mice bearing pancreatic carcinoma xenografts, deltarasin has been shown to reduce tumor growth at a dose of 10 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zimmermann, G., Papke, B., Ismail, S., et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature 497(7451), 638-642 (2013).