1. Protein Tyrosine Kinase/RTK Autophagy Apoptosis PROTAC
  2. Bcr-Abl Src Autophagy Apoptosis Ligands for Target Protein for PROTAC
  3. Dasatinib

Dasatinib (BMS-354825) est un double Bcr-Abl et Src famille tyrosine kinase puissant et oralement actif avec des IC50s de 0,6 nM, 0,8 nM, respectivement. Dasatinib inhibe également Abl, Src, Fyn, c-Kit et c-KitD816V avec des IC50 de 2,8 nM, 79 nM et 37 nM, respectivement. Dasatinib induit également l'apoptose et l'autophagie. Dasatinib présente une activité puissante antitumorale et a le potentiel de traiter la leucémie myéloïde chronique (LMC).

Dasatinib (BMS-354825) ist ein hochwirksamer, ATP-kompetitiver, oral aktiver dualer Src/Bcr-Abl-Inhibitor mit starker Antitumor-Aktivität. Die Ki-Werte von 16 pM und 30 pM für Src bzw. Bcr-Abl.

Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy, and can cross the blood-brain barrier.

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

CAS No. : 302962-49-8

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Customer Review

Based on 168 publication(s) in Google Scholar

Other Forms of Dasatinib:

Top Publications Citing Use of Products

168 Publications Citing Use of MCE Dasatinib

Cell Proliferation/Viability Assay
In Vivo Efficacy Study
WB
ELISA
IF
Cell Migration/Invasion Assay
RT-PCR
Cell Imaging/Staining

    Dasatinib purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Apr;4(4):527-545.  [Abstract]

    Dasatinib (100 nM; 24 h). mRNA relative expression of CDKN2A, IL-6 and IL-8 in si-FOXP1 COV434 treated with fisetin (F), quercetin (Q) and Dasatinib (D).

    Dasatinib purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Apr;4(4):527-545.  [Abstract]

    Dasatinib (100 nM; 24 h). Immunofluorescence staining of Ki67 upon administration of fisetin (F), quercetin (Q) and Dasatinib (D) in COV434 with knockdown of FOXP1.

    Dasatinib purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Apr;4(4):527-545.  [Abstract]

    Dasatinib (100 nM; 24 h). Immunofluorescence staining of γH2AX upon administration of fisetin (F), quercetin (Q) and dasatinib (D) in COV434 with knockdown of FOXP1.

    Dasatinib purchased from MedChemExpress. Usage Cited in: Nat Aging. 2024 Apr;4(4):527-545.  [Abstract]

    Fisetin (10 μM, 24 h), Quercetin (10 μM, 24 h), or Dasatinib (100 nM, 24 h) delayed FOXP1 gene silencing-induced cellular senescence in COV434 cells.

    Dasatinib purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Mar;25(3):493-507.  [Abstract]

    Dasatinib (50 nM; 24 or 48 h) significantly decreases MED8A and D458 cell migration.

    Dasatinib purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Mar;25(3):493-507.  [Abstract]

    Dasatinib (50 nM;24 h-48 h) significantly decreases MED8A cell migration.

    Dasatinib purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2023 Aug 29:14:1250383.  [Abstract]

    Dasatinib hydrochloride (Dasatinib; 20 μM; 2 h) suppressed silica particle (SP)-induced cell death. Bone marrow-derived macrophages (BMDMs) were primed with lipopolysaccharide (LPS) (200 ng/mL) for 6 h. The cells were then treated with 20 µM of bosutinib, dasatinib, PD-161570, or PD-166285 and were stimulated or not stimulated with SPs (1,500 nm in diameter, 300 μg/mL) for 2 h. The cell death rate was determined by measuring lactate dehydrogenase (LDH) activity in the culture supernatant.

    Dasatinib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    YSE450-R and EC109-R cells are treated with 200 nM BIBW 2992 alone or in combination with 100 nM Dasatinib for 48 h.

    Dasatinib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    Resistant cells were treated with the indicated concentrations of afatinib in the presence or absence of 100 nM Dasatinib hydrochloride (Dasatinib) for 72 h, and CCK-8 assays were performed to assess cell viability.

    Dasatinib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    Dasatinib hydrochloride (dasatinib; 15 mg/kg; daily for 21 days) showed anti-cancer activity in the xenograft growth of KYSE450-R and PDX03-R mice.

    Dasatinib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    Dasatinib hydrochloride (dasatinib; 15 mg/kg; daily for 21 days) decreased the expression of phosphorylated S6 and ERK after afatinib combined with dasatinib treatment in xenografts growth of KYSE450-R and PDX03-R mice.

    Dasatinib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    Dasatinib hydrochloride (Dasatinib; 20 μM; 2 h) suppressed silica particle (SP)-induced IL-1α and IL-1β release in BMDMs. Bone marrow-derived macrophages (BMDMs) were primed with lipopolysaccharide (LPS) (200 ng/mL) for 6 h. The cells were then treated with 20 µM of bosutinib, dasatinib, PD-161570, or PD-166285 and were stimulated or not stimulated with SPs (1,500 nm in diameter, 300 μg/mL) for 2 h. IL-1α and IL-1 beta (β) levels in the culture supernatants were measured using enzyme-linked immunosorbent assay (ELISA).

    Dasatinib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    Dasatinib hydrochloride (Dasatinib; 20 μM; 4 h) suppressed SP-induced cell death accompanied by IL-1α and IL-1β release in phorbol 12-myristate 13-acetatetreated macrophage-like THP-1 cells. Phorbol 12-myristate 13-acetate-differentiated THP-1 cells were primed with LPS (50 ng/mL) for 16 h. The cells were then treated with dasatinib (20 µM) and were stimulated or not stimulated with SPs (1,500 nm in diameter, 500 μg/mL) for 4 h.

    Dasatinib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    Dasatinib hydrochloride (Dasatinib; 20 μM; 2 h) suppressed silica particle (SP)-induced cell death. Bone marrow-derived macrophages (BMDMs) were primed with lipopolysaccharide (LPS) (200 ng/mL) for 6 h. The cells were then treated with 20 µM of bosutinib, dasatinib, PD-161570, or PD-166285 and were stimulated or not stimulated with SPs (1,500 nm in diameter, 300 μg/mL) for 2 h. The cell death rate was determined by measuring lactate dehydrogenase (LDH) activity in the culture supernatant.

    Dasatinib purchased from MedChemExpress. Usage Cited in: Biol Pharm Bull. 2017;40(10):1747-1753.  [Abstract]

    Synergistic Decrease Bcl-2 Expression by the Combination of SAHA with Dasatinib in MCF-7 Cells.

    Dasatinib purchased from MedChemExpress. Usage Cited in: Chem Pharm Bull (Tokyo). 2017 Aug 1;65(8):768-775.  [Abstract]

    Changes in Bcl-2 protein expression in MCF-7 cells after treatment with NSC 105014, Dasatinib or ZD1839 alone or in combination for 12 h. Expression of Bcl-2 protein is analyzed by western blotting analysis.

    Dasatinib purchased from MedChemExpress. Usage Cited in: Kawasaki Medical Journal. 43(2):63-78,2017.

    Western blot analysis of effects of Dasatinib (10 or 100nM) on c-Src, p-SrcY416, FAK and p-FAKY861 expression levels in KTC-1 cells and band intensities for p-SrcY416.

    Dasatinib purchased from MedChemExpress. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44.  [Abstract]

    Drug combination effect on phosphorylation of AKT. Expression of phospho-AKT and total AKT in MOLM13 cells treated for 15 minutes with DMSO vehicle, PKC412 (2.5 nM), Dasatinib (165 nM), or a combination of both. Protein lysates are prepared from MOLM13 cells, and are analyzed via immunoblotting with antibodies to phospho-AKT and total AKT.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy, and can cross the blood-brain barrier[1][2].

    IC50 & Target[1]

    Bcr-Abl

    1.0 nM (IC50)

    Src

    0.5 nM (IC50)

    lck

    0.4 nM (IC50)

    yes

    0.5 nM (IC50)

    c-kit

    5.0 nM (IC50)

    PDGFRβ

    28 nM (IC50)

    p38

    100 nM (IC50)

    Her1

    180 nM (IC50)

    Her2

    710 nM (IC50)

    FGFR-1

    880 nM (IC50)

    MEK

    1700 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    2.55 μM
    Compound: Dasatinib
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    [PMID: 38171149]
    ASPC1 IC50
    3.3 μM
    Compound: Dasatinib
    Cytotoxicity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell growth
    Cytotoxicity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell growth
    [PMID: 38848113]
    B16-F10 IC50
    0.74 μM
    Compound: Dasatinib
    Synergistic photodynamic antitumor activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs under 10 J/cm2 light irradiation at 660 nm in presence of chlorin e6 by CCK-8 assay
    Synergistic photodynamic antitumor activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs under 10 J/cm2 light irradiation at 660 nm in presence of chlorin e6 by CCK-8 assay
    [PMID: 37690263]
    B16-F10 IC50
    13.5 μM
    Compound: Dasatinib
    Synergistic photodynamic antitumor activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs under dark condition in presence of chlorin e6 by CCK-8 assay
    Synergistic photodynamic antitumor activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs under dark condition in presence of chlorin e6 by CCK-8 assay
    [PMID: 37690263]
    B16-F10 IC50
    16.42 μM
    Compound: Dasatinib
    Cytotoxicity against mouse B16-F10 cells incubated for 48 hrs under dark condition by CCK-8 assay
    Cytotoxicity against mouse B16-F10 cells incubated for 48 hrs under dark condition by CCK-8 assay
    [PMID: 37690263]
    BaF3 IC50
    0.3 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    0.4 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    1 nM
    Compound: Dasatinib
    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
    1.1 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    1.2 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    2 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    2 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    2.3 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    2.7 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    2.8 nM
    Compound: Dasatinib
    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]
    BaF3 IC50
    3800 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    5200 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    65 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    7.3 nM
    Compound: Dasatinib
    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
    8 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    8 nM
    Compound: Dasatinib
    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
    [PMID: 21481795]
    BaF3 IC50
    > 200 nM
    Compound: Chemical probe: BMS-354825
    Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by methane-thiosulfonate-based CellTiter96 viability analysis
    Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by methane-thiosulfonate-based CellTiter96 viability analysis
    [PMID: 15930265]
    Hep 3B2 GI50
    86 nM
    Compound: Dasatinib
    Growth inhibition of human Hep3B cells after 3 days by MTT assay
    Growth inhibition of human Hep3B cells after 3 days by MTT assay
    [PMID: 18979199]
    HepG2 GI50
    > 50000 nM
    Compound: Dasatinib
    Growth inhibition of human HepG2 cells after 3 days by MTT assay
    Growth inhibition of human HepG2 cells after 3 days by MTT assay
    [PMID: 18979199]
    HepG2 IC50
    1.01 μM
    Compound: Dasatinib
    Synergistic photodynamic antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs under 10 J/cm2 light irradiation at 660 nm in presence of chlorin e6 by CCK-8 assay
    Synergistic photodynamic antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs under 10 J/cm2 light irradiation at 660 nm in presence of chlorin e6 by CCK-8 assay
    [PMID: 37690263]
    HepG2 IC50
    18.2 μM
    Compound: Dasatinib
    Cytotoxicity against human HepG2 cells incubated for 48 hrs under dark condition by CCK-8 assay
    Cytotoxicity against human HepG2 cells incubated for 48 hrs under dark condition by CCK-8 assay
    [PMID: 37690263]
    HepG2 IC50
    74.75 μM
    Compound: Dasatinib
    Synergistic photodynamic antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs under dark condition in presence of chlorin e6 by CCK-8 assay
    Synergistic photodynamic antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs under dark condition in presence of chlorin e6 by CCK-8 assay
    [PMID: 37690263]
    Huh-7 GI50
    1972 nM
    Compound: Dasatinib
    Growth inhibition of human Huh-7 cells after 3 days by MTT assay
    Growth inhibition of human Huh-7 cells after 3 days by MTT assay
    [PMID: 18979199]
    MCF7 IC50
    > 10 μM
    Compound: Dasatinib
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth
    [PMID: 38848113]
    MDA-MB-231 IC50
    0.157 μM
    Compound: Dasatinib
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 38070430]
    NCI-H1975 IC50
    1.26 μM
    Compound: Dasatinib
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
    [PMID: 38171149]
    PLC-PRF-5 GI50
    15 nM
    Compound: Dasatinib
    Growth inhibition of human PLC-PRF-5 cells after 3 days by MTT assay
    Growth inhibition of human PLC-PRF-5 cells after 3 days by MTT assay
    [PMID: 18979199]
    Vero C1008 EC50
    5.4 μM
    Compound: Dasatinib
    Antiviral activity against MERS-CoV infected in african green monkey Vero E6
    Antiviral activity against MERS-CoV infected in african green monkey Vero E6
    [PMID: 37597435]
    In Vitro

    Dasatinib demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively[1].
    Dasatinib shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively[1].

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

    In Vivo

    Dasatinib (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels[1].
    Dasatinib (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%[1].

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

    Animal Model: Nude mice bearing K562 xenografts
    Dosage: 5 mg/kg and 50 mg/kg
    Administration: Oral administration on a 5 day on and 2 day off schedule.
    Result: Showed partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.
    Animal Model: Sprague-Dawley Rats
    Dosage: 10 mg/kg (Pharmacokinetic Analysis)
    Administration: Oral and i.v.
    Result: Cmax of 13.2 and 0.5 μM for i.v. and oral, respectively.
    Clinical Trial
    Molecular Weight

    488.02

    Formula

    C22H26ClN7O2S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CN=C(S1)NC2=NC(C)=NC(N3CCN(CC3)CCO)=C2)NC4=C(C=CC=C4Cl)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (204.91 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0491 mL 10.2455 mL 20.4910 mL
    5 mM 0.4098 mL 2.0491 mL 4.0982 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

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    In Vivo:

    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.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 50 mg/mL (102.45 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  20% SBE-β-CD in Saline

      Solubility: 2 mg/mL (4.10 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
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    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.85%

    References

    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 2.0491 mL 10.2455 mL 20.4910 mL 51.2274 mL
    5 mM 0.4098 mL 2.0491 mL 4.0982 mL 10.2455 mL
    10 mM 0.2049 mL 1.0245 mL 2.0491 mL 5.1227 mL
    15 mM 0.1366 mL 0.6830 mL 1.3661 mL 3.4152 mL
    20 mM 0.1025 mL 0.5123 mL 1.0245 mL 2.5614 mL
    25 mM 0.0820 mL 0.4098 mL 0.8196 mL 2.0491 mL
    30 mM 0.0683 mL 0.3415 mL 0.6830 mL 1.7076 mL
    40 mM 0.0512 mL 0.2561 mL 0.5123 mL 1.2807 mL
    50 mM 0.0410 mL 0.2049 mL 0.4098 mL 1.0245 mL
    60 mM 0.0342 mL 0.1708 mL 0.3415 mL 0.8538 mL
    80 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6403 mL
    100 mM 0.0205 mL 0.1025 mL 0.2049 mL 0.5123 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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