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DCC-2036

Cat. No. M1702
DCC-2036 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 180 In stock
50mg USD 720 In stock
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Quality Control
Biological Activity

DCC-2036, known as the lead "switch-control" inhibitor, potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant CML-resistance mutants, including T315I. DCC-2036 inhibits BCR-ABL1 (T315I)-expressing cell lines, prolongs survival in mouse models of T315I mutant CML and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing T315I in vitro and in vivo, supporting its clinical development in TKI-resistant Ph (+) leukemia.

Protocol
Cell Experiment
Cell lines Ba/F3 cells or primary Ph+ leukemia cells
Preparation method Cell Proliferation Assays
Ba/F3 cells (3×103 cells/well) or primary Ph+ leukemia cells (5×104 cells/well) were plated in triplicate in 96-well plates containing test compounds. After 72h, viable cells were quantified by resazurin (O’Brien et al., 2000) or MTT (Roumiantsev et al., 2002) assay as described. Results represent an average of at least three independent experiments.
Concentrations 0.1~10 mM
Incubation time 72 h
Animal Experiment
Animal models Allograft and retroviral BM transduction/transplantation mouse models of BCR-ABL1-induced leukemia
Formulation 0.5% CMC/1% Tween-80
Dosages 100 mg/kg once daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 553.59
Formula C30H28FN7O3
CAS Number 1020172-07-9
Purity 98.66%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source PLoS One (2013). Figure 1. DCC-2036
Method Immunoblotting
Cell Lines EOL-1 cells
Concentrations 6 nM
Incubation Time 24 h
Results DCC-2036 effectively decreased the phosphorylated-PDGFRa in BaF3 cells expressing FIP1L1-PDGFRa T674I mutant in a concentration- and time-dependent manner while the total protein level of PDGFRa was not affected.
Rating
References

The BCR-ABL35INS insertion/truncation mutant is kinase-inactive and does not contribute to tyrosine kinase inhibitor resistance in chronic myeloid leukemia.
O'Hare et al. Blood. 2011 Nov 10;118(19):5250-4. PMID: 21908430.

The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile.
Eide et al. Cancer Res. 2011 May 1;71(9):3189-95. PMID: 21505103.

Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Chan et al. Cancer Cell. 2011 Apr 12;19(4):556-68. PMID: 21481795.

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Keywords: DCC-2036 supplier, Src-bcr-Abl, inhibitors

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