1. Metabolic Enzyme/Protease
  2. Proteasome

Delanzomib (Synonyms: CEP-18770)

Cat. No.: HY-10454 Purity: 95.48%
Handling Instructions

Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.

For research use only. We do not sell to patients.
Delanzomib Chemical Structure

Delanzomib Chemical Structure

CAS No. : 847499-27-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 165 In-stock
5 mg USD 150 In-stock
10 mg USD 276 In-stock
50 mg USD 780 In-stock
100 mg USD 1152 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity. IC50 Value: 3.8 nM [1] Target: proteasome in vitro: CEP-18770 and bortezomib showed comparable potency against chymotrypsin-like proteasome activity, cellular inhibitory activity (IC50) values of 3.8 (± 1.0) nM and 3.8 (± 0.4) nM, respectively, CEP-18770 had a 2- to 11-fold lower cytotoxic potency compared with bortezomib against solid tumor cell lines, comparable potency against 2 hematologic tumor cell lines, and a similar spectrum of antiproliferative activity with IC50 values for both compounds of less than 35 nM [1]. in vivo: in MM xenograft models, the addition of CEP-18770 IV to melphalan completely prevented the growth of both melphalan-sensitive and melphalan-resistant tumours. The combination of CEP-18770 IV and bortezomib induced complete regression of bortezomib-sensitive tumours and markedly delayed progression of bortezomib-resistant tumours compared to treatment with either agent alone [2]. Age matched MRL/lpr or NZBWF1 mice with established SLE or LN, respectively, were treated with delanzomib either 3 mg/kg once or twice weekly intravenously or orally at 10 mg/kg [3]. Toxicity: CEP-18770 showed a favourable safety profile with lack of neurotoxicity and linear plasma PK. The definition of the optimal biological dose and schedule of treatment is actively pursued because of the high incidence of skin toxicity of the twice a week schedule [4]. Clinical trial: CEP-18770 in Combination With Lenalidomide and Dexamethasone in Relapsed or Refractory Multiple Myeloma. Phase1/2

Clinical Trial
References
Molecular Weight

413.28

Formula

C₂₁H₂₈BN₃O₅

CAS No.

847499-27-8

SMILES

CC(C)C[[email protected]@H](B(O)O)NC([[email protected]@H](NC(C1=NC(C2=CC=CC=C2)=CC=C1)=O)[[email protected]](O)C)=O

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:
Delanzomib
Cat. No.:
HY-10454
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