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DD 03-171

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Catalog No. T35481Cas No. 2366132-45-6

Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib-resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.

DD 03-171

DD 03-171

😃Good
Catalog No. T35481Cas No. 2366132-45-6
Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib-resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.
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5 mg$1,08035 days
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Product Introduction

Bioactivity
Description
Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.
Chemical Properties
Molecular Weight991.163
FormulaC55H62N10O8
Cas No.2366132-45-6
Relative Density.1.34 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 49.56 mg/mL (50 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.0089 mL5.0446 mL10.0892 mL50.4458 mL
5 mM0.2018 mL1.0089 mL2.0178 mL10.0892 mL
10 mM0.1009 mL0.5045 mL1.0089 mL5.0446 mL
20 mM0.0504 mL0.2522 mL0.5045 mL2.5223 mL
50 mM0.0202 mL0.1009 mL0.2018 mL1.0089 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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Keywords

DD 03171DD 03-171DD 03 171
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