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508942 Prokineticin 2 Antagonist, PKRA7 - CAS 1233926-87-8 - Calbiochem

A cell permeable, brain permeant antagonist of polypeptide chemokine prokineticin 2 receptor (IC₅₀ = 5 nM and 8.2 nM for PKR1 and PKR2, respectively).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: PROK2 Antagonist, PKRA7, Bv8 Antagonist, PKRA7, PK2 Antagonist, PKRA7

Primary Target: PROK2
508942
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1233926-87-8C₂₇H₃₄ClFN₂O₄

Products

Catalogue NumberPackaging Qty/Pack
5089420001 Glass bottle 5 mg
Description
OverviewA cell permeable, brain permeant 3-pyrrolidine carboxamide derivative that acts as an antagonist of polypeptide chemokine prokineticin 2 (PK2) receptor (Bv8, PROK2; IC50 = 5 nM and 8.2 nM for PKR1 and PKR2, respectively). Suppresses the growth of D456MG glioma cell xenografts in nude mice by reducing blood vessel density and blocking angiogenesis via inhibition of PKR1 and PKR2 expressed on endothelial cells. Shown to suppress the growth of AsPC1 and CFPac-1 pancreatic tumor cells in xenograft model of nude mice by reducing macrophage migration and inflitration. Reduces the expression of CCL27, CCR10, CCR4, CCR5, and CCR6 pro-migratory chemokines and chemokine receptors in macrophages. Enhances the efficacy of standard temomolomide in the treatment of glioblastoma and gemcitabine in the treatment of pancreatic cancer in xenograft nude mice models.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number508942
Brand Family Calbiochem®
SynonymsPROK2 Antagonist, PKRA7, Bv8 Antagonist, PKRA7, PK2 Antagonist, PKRA7
References
ReferencesCurtis, V., et al. 2013. PLoS One. 8, e54916.
Product Information
CAS number1233926-87-8
FormColorless semi-solid
Hill FormulaC₂₇H₃₄ClFN₂O₄
Chemical formulaC₂₇H₃₄ClFN₂O₄
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetPROK2
Primary Target IC<sub>50</sub>5 nM
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5089420001 04055977261455

Documentation

Prokineticin 2 Antagonist, PKRA7 - CAS 1233926-87-8 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Curtis, V., et al. 2013. PLoS One. 8, e54916.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision13-June-2014 JSW
SynonymsPROK2 Antagonist, PKRA7, Bv8 Antagonist, PKRA7, PK2 Antagonist, PKRA7
DescriptionA cell permeable, brain permeant 3-pyrrolidine carboxamide derivative that acts as an antagonist of polypeptide chemokine prokineticin 2 (PK2) receptor (Bv8, PROK2; IC50 = 5 nM and 8.2 nM for PKR1 and PKR2, respectively). Suppresses the growth of D456MG glioma cell xenografts in nude mice by reducing blood vessel density and blocking angiogenesis via inhibition of PKR1 and PKR2 expressed on endothelial cells. Shown to suppress the growth of AsPC1 and CFPac-1 pancreatic tumor cells in xenograft model of nude mice by reducing macrophage migration and inflitration. Reduces the expression of CCL27, CCR10, CCR4, CCR5, and CCR6 pro-migratory chemokines and chemokine receptors in macrophages. Enhances the efficacy of standard temomolomide in the treatment of glioblastoma and gemcitabine in the treatment of pancreatic cancer in xenograft nude mice models.
FormColorless semi-solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1233926-87-8
Chemical formulaC₂₇H₃₄ClFN₂O₄
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesCurtis, V., et al. 2013. PLoS One. 8, e54916.