Cat. No.: HY-10181G

Dasatinib (GMP)

(Synonyms: BMS-354825 (GMP))

Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_i values for Src and Bcr-Abl are 16 pM and 30 pM, respectively. Dasatinib inhibits Bcr-Abl and Src with IC₅₀ values of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.

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CAS No.: 302962-49-8
Formule: C₂₂H₂₆ClN₇O₂S
Masse moléculaire:488.01

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

Dasatinib (GMP) Chemical Structure

CAS No.: 302962-49-8

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
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Références
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Description

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Voir tous les produits spécifiques à Isoform Bcr-Abl :

Abl
Bcr-Abl

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	>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]
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]
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 (t_1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (F_po) in this study is 27%^[1].

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

Chemical Information

CAS No. 302962-49-8
Masse moléculaire 488.01
Formule C₂₂H₂₆ClN₇O₂S
SMILES

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

BMS-354825 (GMP)
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Lombardo L J, et al. Discovery of N-(2-chloro-6-methyl-phenyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1-yl)-2-methylpyrimidin-4-ylamino) thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays[J]. Journal of medicinal chemistry, 2004, 47(27): 6658-6661. [Content Brief]

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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.

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Dasatinib (GMP)

Voir tous les produits spécifiques à Isoform Src

Voir tous les produits spécifiques à Isoform Bcr-Abl

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

Dasatinib (GMP) Related Classifications

HY-10181G Related Classifications