538340 CK1δ Inhibitor, SR-1277 - Calbiochem

538340
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₁H₁₉N₉O₃S

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      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.38340.0001
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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
          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.