538340 CK1δ Inhibitor, SR-1277 - Calbiochem

538340
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₁H₁₉N₉O₃S

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable, brain permeant, purine derivative that acts as a potent, ATP-competitive inhibitor of CK1δ (IC50 = 49 nM; Ki = 69 nM). Inhibits CK1δ, FLT3, Cdk6/Cyclin D3 and Cdk9/Cyclin K, but with reduced potency (IC50 = 260, 305, 311, and 260 nM, respectively). Suppresses the proliferation of cerebellar granule cell progenitors (GCPs), without inducing cell death. Also reduces the expression on sonic hedgehog (Shh; 75 ng/ml)-induced Ccna1, Ccnb1, Ccnd2, Ccne1, Cdkn1a, and Cdkn1b mRNA in GCPs (~ 100 nM). Displays anti-proliferative effect in A375 melanoma cells (EC50 = 22 nM in MTT assay) and in DAOY and D283 human medulloblastoma cell lines. Decreases proliferation of subcutaneously injected Ptch1+/- tumor cells allografts in mice (20 mg/kg, b,i.d).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number538340
      Brand Family Calbiochem®
      Synonyms2-morpholino-N-((4-nitro-1H-benzo[d]imidazol-2-yl)methyl)-9-(thiophen-3-yl)-9H-purin-6-amine, ML177, Casein Kinase 1δ Inhibitor, SR-1277
      References
      ReferencesBibian, M., et al. 2013. Bioorg. Med. Chem. Lett. 23, 4374.
      Penas, C., et al. 2015. Cell. Rep. 11, 249.
      Product Information
      FormOrange yellow solid
      Hill FormulaC₂₁H₁₉N₉O₃S
      Chemical formulaC₂₁H₁₉N₉O₃S
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCK1δ
      Primary Target IC<sub>50</sub>49 nM for CK&delta
      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 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

      Documentation

      CK1δ Inhibitor, SR-1277 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Bibian, M., et al. 2013. Bioorg. Med. Chem. Lett. 23, 4374.
      Penas, C., et al. 2015. Cell. Rep. 11, 249.
      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.

      Revision16-March-2017 JSW
      Synonyms2-morpholino-N-((4-nitro-1H-benzo[d]imidazol-2-yl)methyl)-9-(thiophen-3-yl)-9H-purin-6-amine, ML177, Casein Kinase 1δ Inhibitor, SR-1277
      DescriptionA cell-permeable, brain permeant, purine derivative that acts as a potent, ATP-competitive inhibitor of CK1δ (IC50 = 49 nM; Ki = 69 nM). Inhibits CK1δ, FLT3, Cdk6/Cyclin D3 and Cdk9/Cyclin K, but with reduced potency (IC50 = 260, 305, 311, and 260 nM, respectively). Suppresses the proliferation of cerebellar granule cell progenitors (GCPs), without inducing cell death. Also reduces the expression on sonic hedgehog (Shh; 75 ng/ml)-induced Ccna1, Ccnb1, Ccnd2, Ccne1, Cdkn1a, and Cdkn1b mRNA in GCPs (~ 100 nM). Displays anti-proliferative effect in A375 melanoma cells (EC50 = 22 nM in MTT assay) and in DAOY and D283 human medulloblastoma cell lines. Decreases proliferation of subcutaneously injected Ptch1+/- tumor cells allografts in mice (20 mg/kg, b,i.d).
      FormOrange yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₁H₁₉N₉O₃S
      Purity≥98% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesBibian, M., et al. 2013. Bioorg. Med. Chem. Lett. 23, 4374.
      Penas, C., et al. 2015. Cell. Rep. 11, 249.