Rebastinib
Based on 13 publication(s) in Google Scholar
Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.74%
- CAS. Nr.: 1020172-07-9
- Formel: C30H28FN7O3
- Molecular Weight:553.59
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Rebastinib
More- Nat Commun. 2021 Jan 25;12(1):504. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Clin Invest. 2026 Jan 6;136(4):e193758. [Abstract]
- J Exp Clin Cancer Res. 2022 Apr 21;41(1):149. [Abstract]
- Brain. 2025 May 13;148(5):1723-1739. [Abstract]
- J Exp Med. 2026 May 4;223(5):e20251374. [Abstract]
- J Med Chem. 2015 Jan 8;58(1):466-79. [Abstract]
- J Cell Sci. 2026 May 28:jcs.264977. [Abstract]
- Anticancer Drugs. 2024 Jan 1;35(1):46-54. [Abstract]
- Res Sq. 2025 Sep 1.
- bioRxiv. 2025 August 23.
- University of Washington. 2025.
- Patent. US20170349880A1.
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Histological Imaging/Staining
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Histological Imaging/Staining
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Histological Imaging/Staining
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Histological Imaging/Staining
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Cell Imaging/Staining
Biologische Aktivität
IC50: 0.75±0.11 nM (ABL1WT), 2±0.3 nM (FLT3), 4±0.3 nM (KDR), 6±0.3 nM (TIE2), 34±6 nM (SRC)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
120 nM
Compound: DCC-2036
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Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
127 nM
Compound: DCC-2036
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
13 nM
Compound: DCC-2036
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Antiproliferative activity against mouse BAF3 cells harboring wild type BCR-ABL measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BAF3 cells harboring wild type BCR-ABL measured after 72 hrs by MTT assay
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[PMID: 35551036] |
| BaF3 | IC50 |
13 nM
Compound: DCC-2036
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Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
14 nM
Compound: DCC-2036
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
150 nM
Compound: DCC-2036
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Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
19 nM
Compound: DCC-2036
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Antiproliferative activity against mouse BAF3 cells harboring BCR-ABL T315I mutant measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BAF3 cells harboring BCR-ABL T315I mutant measured after 72 hrs by MTT assay
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[PMID: 35551036] |
| BaF3 | IC50 |
19 nM
Compound: DCC-2036
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Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
24 nM
Compound: DCC-2036
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Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
3500 nM
Compound: DCC-2036
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Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay
Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
36 nM
Compound: DCC-2036
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Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
39 nM
Compound: DCC-2036
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Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
5.4 nM
Compound: DCC-2036
|
Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
51 nM
Compound: DCC-2036
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
56 nM
Compound: DCC-2036
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
6 nM
Compound: DCC-2036
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
81 nM
Compound: DCC-2036
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
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[PMID: 21481795] |
| BaF3 | IC50 |
98 nM
Compound: DCC-2036
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| K562 | IC50 |
5.5 nM
Compound: DCC-2036
|
Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay
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[PMID: 21481795] |
Rebastinib potently (IC50 0.82 nM) inhibits u-ABL1native, which is thought to exist predominantly in the inactive type II conformation. In addition, Rebastinib also strongly inhibits p-ABL1native (IC50 2 nM), which more readily adopts an active, Type I conformation[1].
Rebastinib potently inhibits both u-ABL1T315I (IC50 5 nM) and p-ABL1T315I (IC50 4 nM), both of which exist predominately in the Type I conformation due to stabilization of an activating hydrophobic spine by the T315I mutation[1].
In addition to ABL1, Rebastinib also inhibits the SRC family kinases LYN, SRC, FGR, and HCK, and PDGFRα, and PDGFRβ with IC50 of 29±1, 34±6, 38±1, 40±1, 70±10 and 113±10 nM, respectively. Notably, Rebastinib spared c-KIT (IC50 481 nM)[1].
Rebastinib effectively inhibits the proliferation of Ba/F3 cells expressing native BCR-ABL1native (IC50 5.4 nM). Rebastinib also inhibits proliferation of the Ph+ cell line K562 (IC50 5.5 nM)[1].
Rebastinib also inhibits proliferation of several common TKI-resistant mutants of BCR-ABL1, including G250E, Q252H, Y235F, E255K, V299L, F317L, and M351T, at IC50s ranging from 6-150 nM. Rebastinib effectively inhibits autophosphorylation of BCR-ABL1native (IC50 29 nM) and BCR-ABL1T315I (IC50 18 nM), as well as the phosphorylation of STAT5 in both cell lines (IC50 28 nM and 13 nM, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Treatment of mice bearing Ba/F3-BCR-ABL1T315I leukemia cells with Rebastinib at 100 mg/kg once daily by oral gavage significantly prolonged their survival, while STI571 at 100 mg/kg twice daily is ineffective[1].
In this aggressive allograft model, Rebastinib is as effective for treatment of BCR-ABLT315I leukemia as STI571 at 100 mg/kg twice daily in BCR-ABL1native leukemia, and reduces the leukemia cell burden in the spleens of treated mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1020172-07-9
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Appearance Solid
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Molecular Weight 553.59
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Formel C30H28FN7O3
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Color White to off-white
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SMILES
CC(C)(C)C1=NN(C(NC(NC2=C(F)C=C(OC3=CC(C(NC)=O)=NC=C3)C=C2)=O)=C1)C4=CC=C5C(C=CC=N5)=C4
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Synonyms
DCC-2036
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
Caveolae-mediated Tie2 signaling contributes to CCM pathogenesis in a brain endothelial cell-specific Pdcd10-deficient mouse model. [Abstract]2021 Jan 25;12(1):504. PMID: 33495460
Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]
Rebastinib (1 μM) blunted increased EC sprouting and enlarged lumen formation induced by CCM3 knockdown.
Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]
Rebastinib (10 μg/g; s.c.; 11 d) diminished the CCM lesions induced by Ccm3 deletion as visualized by whole-brain imaging and H&E staining compared to vehicle treatment in Pdcd10BECKO mice.
Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]
Rebastinib (10 μg/g; s.c.; once daily for 11 d) normalized the NG2+ pericyte coverage of CD31+ microvessels in Pdcd10BECKO mice.
Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]
Rebastinib (10 μg/g; s.c.; once daily for 11 d) caussed very fewer CCM lesions in brain of Pdcd10BECKO mice compared to vehicle group even at age of 2 months.
Rebastinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jan 25;12(1):504. [Abstract]
Rebastinib (10 μg/g; s.c.; 11 d) increased pericyte density and diminished pericyte-free caverns in Pdcd10BECKO mice.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Clin Invest
Vessels encapsulating tumor clusters promote noninvasive metastasis of hepatocellular carcinoma by shaping an immunosuppressive microenvironment. [Abstract]2026 Jan 6;136(4):e193758. PMID: 41493808 -
J Exp Clin Cancer Res
CDK16 promotes the progression and metastasis of triple-negative breast cancer by phosphorylating PRC1. [Abstract]2022 Apr 21;41(1):149. PMID: 35449080 -
Brain
Three-dimensional tissue engineered skeletal muscle modelling facioscapulohumeral muscular dystrophy. [Abstract]2025 May 13;148(5):1723-1739. PMID: 39556762 -
J Exp Med
2026 May 4;223(5):e20251374. PMID: 41891922 -
J Med Chem
Conformational analysis of the DFG-out kinase motif and biochemical profiling of structurally validated type II inhibitors. [Abstract]2015 Jan 8;58(1):466-79. PMID: 25478866 -
J Cell Sci
2026 May 28:jcs.264977. PMID: 42206576 -
Anticancer Drugs
2024 Jan 1;35(1):46-54. PMID: 37449977 -
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Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (90.32 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Ba/F3 cells (3×103 cells/well) or primary Ph+ leukemia cells (5×104 cells/well) are plated in triplicate in 96-well plates containing test compounds (e.g., Rebastinib (DCC-2036)). After 72h, viable cells are quantified by resazurin or MTT assay. Results represent an average of at least three independent experiments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Ba/F3 cells (1×106) transformed to interleukin-3 independence by transduction with either BCR-ABL1native or BCR-ABL1T315I retrovirus are injected intravenously into syngeneic Balb/c recipients. Beginning day 3 post-injection, mice are treated with STI571 (100 mg/kg in water twice daily via oral gavage) or with Rebastinib (DCC-2036) (100 mg/kg in 0.5% CMC/1% Tween-80, once daily via oral gavage) or with vehicle (0.5% CMC/1% Tween-80) alone. For induction of CML-like leukemia, bone marrow (BM) from male Balb/c donor mice is harvested 4d after intravenous administration of 150 mg/kg 5-FU, transduced with BCR-ABL1T315I retrovirus, and 5×105 cells injected intravenously into sublethally irradiated (400 cGy) Balb/c recipients. Beginning at d5 post-transplant, cohorts are treated once daily by oral gavage with vehicle alone, or Rebastinib (DCC-2036) at 100 mg/kg. For induction of B-cell acute lymphoblastic leukemia, BM from donors not pretreated with 5-FU is transduced once with BCR-ABL1T315I retrovirus and 1×106 cells injected into sublethally irradiated Balb/c recipients. Beginning at d8 post-transplant, cohorts are treated twice daily by oral gavage with vehicle alone, with Rebastinib (DCC-2036) at 60 mg/kg, with STI571 at 100 mg/kg (in water), or with BMS-354825 at 10 mg/kg (in 80 mM citric acid pH 3.1).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8064 mL | 9.0320 mL | 18.0639 mL | 45.1598 mL |
| 5 mM | 0.3613 mL | 1.8064 mL | 3.6128 mL | 9.0320 mL | |
| 10 mM | 0.1806 mL | 0.9032 mL | 1.8064 mL | 4.5160 mL | |
| 15 mM | 0.1204 mL | 0.6021 mL | 1.2043 mL | 3.0107 mL | |
| 20 mM | 0.0903 mL | 0.4516 mL | 0.9032 mL | 2.2580 mL | |
| 25 mM | 0.0723 mL | 0.3613 mL | 0.7226 mL | 1.8064 mL | |
| 30 mM | 0.0602 mL | 0.3011 mL | 0.6021 mL | 1.5053 mL | |
| 40 mM | 0.0452 mL | 0.2258 mL | 0.4516 mL | 1.1290 mL | |
| 50 mM | 0.0361 mL | 0.1806 mL | 0.3613 mL | 0.9032 mL | |
| 60 mM | 0.0301 mL | 0.1505 mL | 0.3011 mL | 0.7527 mL | |
| 80 mM | 0.0226 mL | 0.1129 mL | 0.2258 mL | 0.5645 mL |