Cat. No.: HY-13024A

Rebastinib tosylate

(Synonyms: DCC-2036 tosylate)

13 Cited Publications

Customer Review

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.

For research use only. We do not sell to patients.

CAS No.: 1033893-29-6
Formula: C₃₇H₃₆FN₇O₆S
Molecular Weight:725.79

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

Rebastinib tosylate Chemical Structure

CAS No.: 1033893-29-6

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Purity & Documentation
References
Calculators
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Biological Activity

Description

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

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

All Cytochrome P450 Isoforms :

All Tie Isoforms :

Tie1
Tie2

All FOXO Isoforms :

FOXO1
FOXO3

All Src Isoforms :

In Vitro

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

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.

In Vivo

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].
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].
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].
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].
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)^[4].

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).

Chemical Information

CAS No. 1033893-29-6
Molecular Weight 725.79
Formula 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
Synonyms

DCC-2036 tosylate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Rebastinib tosylate

13 Cited Publications

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Rebastinib tosylate

Publications Citing Use of MedChemExpress (MCE) Rebastinib tosylate

All Bcr-Abl Isoforms

All Cytochrome P450 Isoforms

All Tie Isoforms

All FOXO Isoforms

All Src Isoforms

Biological Activity

Chemical Information

Publications (13)

Purity & Documentation

References

Calculators

Help & FAQs

Rebastinib tosylate Related Classifications

HY-13024A Related Classifications