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555562 Rho Kinase Inhibitor XIII, RKI-1447 - Calbiochem

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

Synonyms: 1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Methanesulfonate, ROCK Inhibitor XIII, 1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Mesylate

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555562
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Overview

Replacement Information

Products

Catalogue NumberPackaging Qty/Pack
555562-10MGCN Glass bottle 10 mg
Description
OverviewA cell-permeable pyridylthiazolyl-urea that acts as a potent, ATP site-targeting, Rho Kinase inhibitor (IC50 = 14.5 and 6.2 nM against ROCK1 and ROCK2, respectively), displaying much reduced potency against PKA, PKN1/PRK1, p70S6K/RPS6kB1, AKT1, MRCKa/CDC42BPA (85.5%, 80.5%, 61.9%, 56.0%, and 50.4% inhibition, respectively, by 1 µM RKI-1447) or 15 other kinases. Selectively inhibits ROCK-dependent, but not mTORC2-dependent, cellular phosphorylations (effective conc. 0.1 to 1 µM in MDA-MB-231, MDA-MB-468, and H1299 cultures). Shown to be efficacious in suppressing established tumor expansion in a murine ErbB2 mammary cancer model (200 mg/kg/day i.p.) in vivo.
Catalogue Number555562
Brand Family Calbiochem®
Synonyms1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Methanesulfonate, ROCK Inhibitor XIII, 1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Mesylate
References
ReferencesPatel, R.A., et al. 2012. Cancer Res. 72, 5025.
Product Information
FormYellowish white solid
Hill FormulaC₁₆H₁₄N₄O₂S • CH₃SO₃H
Chemical formulaC₁₆H₁₄N₄O₂S • CH₃SO₃H
Hygroscopic Hygroscopic
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetRho kinases 1 & 2
Primary Target IC<sub>50</sub>14.5 and 6.2 nM against ROCK1 and ROCK2, respectively
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 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
555562-10MGCN 04055977268485

Documentation

Rho Kinase Inhibitor XIII, RKI-1447 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Rho Kinase Inhibitor XIII, RKI-1447 - Calbiochem Certificates of Analysis

TitleLot Number
555562

References

Reference overview
Patel, R.A., et al. 2012. Cancer Res. 72, 5025.
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.

Revision12-April-2013 JSW
Synonyms1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Methanesulfonate, ROCK Inhibitor XIII, 1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Mesylate
DescriptionA cell-permeable pyridylthiazolyl-urea that acts as a potent, ATP site-targeting, Rho Kinase inhibitor (IC50 = 14.5 and 6.2 nM against ROCK1 and ROCK2, respectively), displaying much reduced potency against PKA, PKN1/PRK1, p70S6K/RPS6kB1, AKT1, MRCKa/CDC42BPA (85.5%, 80.5%, 61.9%, 56.0%, and 50.4% inhibition, respectively, at 1 µM) and little or no activity against 15 other kinases (IC50 >1 µM). Selectively inhibits ROCK-dependent MLC-2 Ser19 and MYPT-1 Thr696 phosphorylations (effective conc. 0.1 to 1 µM in MDA-MB-231, MDA-MB-468, and H1299 cultures), but not mTORC2-dependent Akt Ser473, PAK-dependent Mek Ser298, or S6K-dependent S6 Ser240/244 phosphorylations (up to 10 µM in MDA-MB-231 cells). Shown to inhibit MDA-MB-231 invasion (by 53% and 85%, respectively, with 1 and 10 µM inhibitor) and anchorage-independent colony formation (IC50 = 709 nM) in vitro and be efficacious in suppressing established tumor expansion in a murine ErbB2 mammary cancer model (8.8% vs. 68.3% average tumor size expansion in 14 days, respectively, with or without treatment; 14 dailly i.p. doses at 200 mg/kg) in vivo.
FormYellowish white solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₆H₁₄N₄O₂S • CH₃SO₃H
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesPatel, R.A., et al. 2012. Cancer Res. 72, 5025.