製品番号: HY-13024A

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Rebastinib tosylate

Name: Rebastinib tosylate
Brand: MedChemExpress
SKU: HY-13024A
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(別名: DCC-2036 tosylate)

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Rebastinib tosylate (DCC-2036 tosylate) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC₅₀ values of 0.8 nM and 4 nM against Abl1^WT and Abl1^T315I, respectively. Rebastinib tosylate potently inhibits CYP2C8 (IC₅₀ = 0.0533 μM) and CYP2C9 (IC₅₀ = 2.54 μM). Rebastinib tosylate allosterically inhibits Tie2 with an IC₅₀ of 0.63 nM. Rebastinib tosylate inhibits the transcriptional activity of FoxO1. Rebastinib tosylate inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib tosylate induces Apoptosis. Rebastinib tosylate exerts anti-tumor activity in breast cancer. Rebastinib tosylate exerts anti-angiogenic effects. Rebastinib tosylate increases myotube diameter and improves reduced contractility. Rebastinib tosylate can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia.

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CAS 番号: 1033893-29-6
分子式: C₃₇H₃₆FN₇O₆S
分子量:725.79

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (311 KB)

Rebastinib tosylate 構造式

CAS 番号: 1033893-29-6

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Other In-stock Forms of Rebastinib tosylate

Rebastinib

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
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Publications (13)
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製品説明

IC₅₀ & Target

^[1]^[2]^[4]

CYP2C8

0.0533 μM (IC₅₀)

CYP2C9

2.54 μM (IC₅₀)

Tie2

0.63 nM (IC₅₀)

Abl1^WT

0.8 nM (IC₅₀)

Abl1^T315I

4 nM (IC₅₀)

FOXO1

Bcr-Abl アイソフォーム固有の製品をすべて表示 :

Abl
Bcr-Abl

Cytochrome P450 アイソフォーム固有の製品をすべて表示 :

Tie アイソフォーム固有の製品をすべて表示 :

Tie1
Tie2

FOXO アイソフォーム固有の製品をすべて表示 :

FOXO1
FOXO3

Src アイソフォーム固有の製品をすべて表示 :

体外実験

Anti-cancerApoptosisLocal Vascular RegulationProtein/Amino Acid MetabolismOthers

Anti-cancer

Rebastinib (10^-10 M-10^-4 M; 72 h) tosylate potently inhibits the proliferation of breast cancer MCF7 and MDA-MB-231 cells. After 72 h of incubation, its IC₅₀ is 2.22 μM against MCF7 cells and 1.63 μM against MDA-MB-231 cells^[1].
Rebastinib tosylate potently inhibits multiple forms of recombinant ABL1 kinase, including the drug-resistant ABL1^T315I and ABL1^H396P mutants, via a non-ATP-competitive mechanism. It exhibits a prolonged kinase residence time and also inhibits a specific subset of other kinases^[4].

Anti-cancer

Apoptosis

Rebastinib (0.5-8.0 μM; 48 h) tosylate induces dose-dependent apoptosis in MCF7 and MDA-MB-231 cells after 48 h of incubation; the total apoptosis rate reaches 16.87% in MCF7 cells at a concentration of 8.0 μM, and 21.62% in MDA-MB-231 cells at a concentration of 6.4 μM^[1].

Local Vascular Regulation

Rebastinib (multiple concentrations) tosylate inhibits Ang1-induced HUVEC migration with an IC₅₀ of 0.022 nM^[2].

Protein/Amino Acid Metabolism

Rebastinib (0.1-3 μM; 24 h) tosylate dose-dependently inhibits the Dexamethasone (HY-14648)-induced upregulation of atrophy-related genes (atrogin-1, MuRF-1) and C/EBPβ mRNA, and modulates the mRNA levels of FoxO1/FoxO3 in C2C12 myotubes^[3].
Rebastinib (1 μM; 24 h) tosylate reduces atrogin-1 protein levels in C2C12 myotubes without altering the phosphorylation status of FoxO1 or FoxO3^[3].

Others

Rebastinib (0.3-30 μM) tosylate exerts no significant inhibitory effect on hERG potassium channel currents in HEK 293 cells, with a maximum average inhibition rate of 31.50% at 30 μM^[1].
Rebastinib (24 h) tosylate potently inhibits the transcriptional activity of FoxO1 in HEK293T cells, with an IC₅₀ of 2.1 × 10^-7 M^[3].
Rebastinib (5-45 min) tosylate potently inhibits CYP2C8 (IC₅₀=0.0533 μM) and CYP2C9 (IC₅₀=2.54 μM), whereas it exhibits only extremely weak inhibition or no inhibition against CYP1A2, CYP2B6, CYP2C19, CYP2D6, and CYP3A4 at concentrations up to 40 μM^[1].
Rebastinib tosylate potently inhibits recombinant non-phosphorylated Tie2 kinase, with an IC₅₀ of 0.63 nM and a dissociation half-life as long as 10 h^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

human breast carcinoma MCF7, MDA-MB-231 cell lines
Concentration:

10^-10 M-10^-4 M
Incubation Time:

72 h
Result:

Inhibited cell proliferation in both cell lines in a concentration-dependent manner, with an IC₅₀ of 2.22 μM for MCF7 cells and 1.63 μM for MDA-MB-231 cells.

Apoptosis Analysis^[1]

Cell Line:

human breast carcinoma MCF7, MDA-MB-231 cell lines
Concentration:

0.5-8.0 μM (MCF7 cells); 0.8-6.4 μM (MDA-MB-231 cells)
Incubation Time:

48 h
Result:

Induced dose-dependent apoptosis in both cell lines.
In MDA-MB-231 cells, total apoptosis increased from 7.95% (control) to 9.8% (0.8 μM), 9.95% (1.6 μM), and 21.62% (6.4 μM), driven primarily by increases in early-stage apoptosis.
In MCF7 cells, total apoptosis increased from 6.88% (control) to 8.2% (0.5 μM), 10.91% (2.0 μM), and 16.87% (8.0 μM), with increases in both early and late-stage apoptosis.

Real Time qPCR^[3]

Cell Line:

mouse C2C12 skeletal muscle myotubes
Concentration:

0.1-3 μM (co-treated with 1 μM DEX)
Incubation Time:

24 h
Result:

Significantly and dose-dependently reduced DEX-induced upregulation of atrogin-1, MuRF-1, and C/EBPβ mRNA.
Decreased basal FoxO1 mRNA levels and the DEX-induced increase in FoxO3 mRNA levels.

Western Blot Analysis^[3]

Cell Line:

mouse C2C12 skeletal muscle myotubes
Concentration:

1 μM (co-treated with 1 μM DEX)
Incubation Time:

24 h
Result:

Significantly reduced DEX-increased atrogin-1 protein levels.
Did not alter levels of total FoxO1, phosphorylated FoxO1, total FoxO3, or phosphorylated FoxO3 compared to DEX-treated vehicle controls.

体内実験

Anti-cancerInnate ImmunityLocal Vascular Regulation

Anti-cancer

Rebastinib (150 mg/kg; intravenous injection; single dose) tosylate exerts no significant inhibitory effect on the growth of MDA-MB-468 triple-negative breast cancer xenografts in female SCID mice, with only reversible body weight changes observed^[1].
Rebastinib tosylate (100 mg/kg; p.o.; once daily) significantly prolongs the survival and reduces the leukemia burden of Balb/c mice with allogeneic transplants of Ba/F3 cells expressing BCR-ABL1^T315I^[4].
Rebastinib tosylate (100 mg/kg; p.o.; once daily) significantly prolongs the survival of Balb/c mice with BCR-ABL1^T315I-induced chronic myeloid leukemia-like myeloproliferative neoplasms and reduces their circulating white blood cell counts^[4].
Rebastinib tosylate (150 mg/kg; intravenous injection; single dose) produces a statistically significant 44.54% inhibition of MDA-MB-231 triple-negative breast cancer xenograft growth in female SCID mice, with reversible body weight changes^[1].
Tosylate of Rebastinib (60 mg/kg; p.o.; twice daily) significantly prolongs the survival of Balb/c mice with BCR-ABL1^T315I-induced B-cell acute lymphoblastic leukemia (B-ALL), and its therapeutic efficacy is superior to that of imatinib and dasatinib^[4].

Anti-cancer

Innate Immunity

Local Vascular Regulation

Combination of tosylate salt of Rebastinib (10 mg/kg; p.o.; daily; twice weekly; once weekly) with Eribulin (HY-13442) reduces primary breast tumor growth by 75%, inhibits lung metastasis by 72%, and prolongs survival in mice, while reducing Tie2⁺macrophage infiltration and impairing TMEM-mediated intravasation of tumor cells^[2].
Tosylate of Rebastinib (10 mg/kg; p.o.; once daily; for 4 consecutive weeks) reduces hepatic micrometastases by 75% in PNET models, while decreasing Tie2⁺macrophage infiltration, perfused microvessel density, and promoting vascular maturation, without affecting the growth of primary tumors^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

SCID (female, 5 weeks old, triple-negative breast cancer xenograft via subcutaneous injection of 5×10⁶ MDA-MB-231 cells)^[1]
Dosage:

150 mg/kg
Administration:

i.v.; single dose
Result:

Achieved a statistically significant tumor growth suppressive rate of 44.54% (p<0.05) compared to control.
Caused a maximum 12% body weight loss by day 28, which was recovered by day 38 with a net 6% weight gain.

Animal Model:

SCID (female, 5 weeks old, triple-negative breast cancer xenograft via subcutaneous injection of 5×10⁶ MDA-MB-468 cells)^[1]
Dosage:

150 mg/kg
Administration:

i.v.; single dose
Result:

Showed no significant tumor growth suppression compared to control.
Caused a maximum 8% body weight loss by day 28, which was recovered by day 38 with a net 7.7% weight gain.

Animal Model:

FVB/NJ (female)^[2]
Dosage:

10 mg/kg
Administration:

p.o.; daily; twice weekly; once weekly
Result:

Reduced primary tumor growth by 75% (TGI 75%).
Produced an additive effect with paclitaxel, reducing tumor growth by 90% (TGI 90%).
Reduced lung metastases by 72%; in combination with paclitaxel, reduced lung metastases by 93%.
Extended mouse median survival to at least 196-200 days when combined with eribulin after primary tumor resection, compared with 54 days for eribulin alone and 84 days for vehicle.
Significantly decreased total macrophages and Tie2+ macrophages in tumor tissue and stroma.
Counteracted paclitaxel-induced increases in total macrophages, Tie2+ macrophages, and CD31+ microvessel density, reducing microvessel density to below vehicle levels.
Reduced vascular permeability (extravascular dextran area/CD31 area decreased by ~70%).
Increased vascular ZO-1 staining intensity relative to CD31.
Reduced normalized circulating tumor cells (CTCs/mL blood) by ~75%, impairing TMEM function without altering TMEM density.

Animal Model:

C57Bl6/6J/RIP1-Tag2 (male, 11.5-12.5 weeks old)^[2]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 4 weeks
Result:

Did not detectably inhibit primary pancreatic insulinoma growth, but significantly reduced liver micrometastases by 75% compared with vehicle.
Reduced Tie2 staining in PNET tumors; total macrophage (F4/80+ area) levels were unchanged, but intratumoral Tie2+ macrophages (F4/80+/Tie2+ area percentage) were significantly decreased.
Significantly reduced protumoral Mrc1+/F4/80+ macrophages at the tumor invasive front and decreased the density of perfused (lectin-positive) blood vessels in PNET tumors.
Increased vascular maturation by increasing the proportion of pericyte-covered (Ng2+) blood vessels.

Animal Model:

Balb/c mice (syngeneic recipients)^[4]
Dosage:

100 mg/kg
Administration:

p.o.; once daily
Result:

Achieved circulating plasma levels exceeding 12 μM for up to 24 hours.
Inhibited BCR-ABL1ᵀ³¹⁵ᴵ signaling (phospho-STAT5, phospho-BCR-ABL1) for up to 8 hours in bone marrow and spleen leukemia cells.
Significantly prolonged mouse survival, with survival superior to imatinib at 100 mg/kg twice daily.
Reduced leukemia cell burden in spleens (spleen weight difference was borderline significant, p=0.06).

Animal Model:

Balb/c mice (male donors, sublethally irradiated recipients)^[4]
Dosage:

100 mg/kg
Administration:

p.o.; once daily
Result:

Prolonged median mouse survival from 20 days to 32 days (p=0.007, Wilcoxon test).
Significantly reduced circulating leukocyte counts on day 20 post-transplant (p=0.0002, unpaired t-test).

Animal Model:

Balb/c mice (sublethally irradiated recipients)^[4]
Dosage:

60 mg/kg
Administration:

p.o.; twice daily
Result:

Significantly prolonged median mouse survival to 47 days, with survival superior to vehicle (p=0.0184), imatinib at 100 mg/kg twice daily (p=0.0474), and dasatinib at 10 mg/kg twice daily (p<0.0001, Wilcoxon tests).

Related Protocols :

化学情報

CAS 番号 1033893-29-6
分子量 725.79
分子式 C₃₇H₃₆FN₇O₆S
SMILES

O=C(NC1=CC(C(C)(C)C)=NN1C2=CC3=CC=CN=C3C=C2)NC4=CC=C(C=C4F)OC5=CC(C(NC)=O)=NC=C5.O=S(O)(C6=CC=C(C)C=C6)=O
別名

DCC-2036 tosylate
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (13)

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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 tosylate 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 tosylate 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 Pdcd10^BECKO mice.

Rebastinib tosylate 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 Pdcd10^BECKO mice.

Rebastinib tosylate 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 Pdcd10^BECKO mice compared to vehicle group even at age of 2 months.

Rebastinib tosylate 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 Pdcd10^BECKO mice.
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

TIE2 links MEKK3-KLF2/4 and PI3K signaling in cerebral cavernous malformation. [Abstract]

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

LRRK2 mutations block NCOA4 trafficking upon iron overload leading to ferroptotic death. [Abstract]

2026 May 28:jcs.264977. PMID: 42206576
Anticancer Drugs

AZD7762 induces CRBN dependent BAG3 degradation through ubiquitin-proteasome pathway. [Abstract]

2024 Jan 1;35(1):46-54. PMID: 37449977
Res Sq

2025 Sep 1.
bioRxiv

2025 August 23.
University of Washington

2025.
Patent

US20170349880A1.

純度とドキュメンテーション

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純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (311 KB)
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元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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SEC-HPLC (2659 KB)
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参考文献

[1]. Feng K, et al. The Suppressive Effect of Rebastinib on Triple-negative Breast Cancer Tumors Involves Multiple Mechanisms of Action. Anticancer research. 2023 Jun;43(6):2609-2624. [Content Brief]

[2]. Harney AS, et al. The Selective Tie2 Inhibitor Rebastinib Blocks Recruitment and Function of Tie2 Macrophages in Breast Cancer and Pancreatic Neuroendocrine Tumors. Molecular cancer therapeutics. 2017 Nov;16(11):2486-2501. [Content Brief]

[3]. Sato T, et al. Rebastinib inhibits FoxO1 activity and reduces dexamethasone-induced atrophy and its-related gene expression in cultured myotubes. The journal of physiological sciences : JPS. 2025 Mar;75(1):100012. [Content Brief]

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

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Rebastinib tosylate

13 Cited Publications

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Rebastinib tosylate

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Rebastinib tosylate

Other In-stock Forms of Rebastinib tosylate

MedChemExpress（MCE）の使用を引用している文献 Rebastinib tosylate

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Publications (13)

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