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302962-49-8 (Dasatinib)

1

Identification

Dasatinib Dasatinib
Name Dasatinib
Formula C22H26ClN7O2S
MW 488.01
CAS No. 302962-49-8
EINECS
Smiles O=C(C1=CN=C(S1)NC2=NC(C)=NC(N3CCN(CC3)CCO)=C2)NC4=C(C=CC=C4Cl)C
Synonyms BMS-354825;Sprycel;BMS354825;BMS 354825; N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide
InChI InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
2

Introduction

Dasatinib(BMS-354825) is a potent and dual Abl/ Src inhibitor IC50 of <1 nM/0.8 nM respectively; also inhibit c-Kit (WT)/c-Kit (D816V) with IC50 of 79 nM/37 nM. IC50 value: <1 nM/0.8 nM(Abl/ Src); 79 nM/37 nM (c-Kit WT/c-Kit D816V) [1] [2] Target: Abl; Src; c-Kit in vitro: Dasatinib is more effective than imatinib in inhibiting the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants, with the exception of T315I.

Background Information

An orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases ......by AOBIOUS INC
Dasatinib (BMS-354825) is a small molecule inhibitor of both the SRC and BCR/ABL tyrosine kinases, with IC50's for the isolated kinases of 0.55 and 3.0 nM, respectively. Dasatinib also inhibits Lyn (IC50 = 8.5 nM) and Src (IC50 = 3.0 nM) kinase activities in vitro using 0.1 mg/mL poly (Glu4-Tyr) as the substrate. Dasatinib has greater potency than imatinib mesylate and has activity against the majority of kinase mutations in imatinib-resistant chronic myeloid leukemia. ......by AbMole BioScience
Dasatinib (BMS-354825) is an oral multi- BCR/ABL and Src family tyrosine kinase inhibitor. The main targets of dasatinib, are BCR/ABL, Src, c-Kit, ephrin receptors, and several other tyrosine kinases, but not erbB kinases such as EGFR or Her2. ......by AdooQ BioScience, LLC
Dasatinib is a potent inhibitor of imatinib-resistant KIT activation loop mutants and induces apoptosis in mast cell and leukemic cell lines expressing these mutations. Dasatinib sensitively inhibits all members of the Src family, including c-Src, Lck,Fyn, and Yes (IC50 < 1.1nmol/L). At higher concentrations (3 to 28 nmol/L), dasatinib also inhibits the Src kinases Abl, c-Kit, PDGFR, and EphA2. ......by Affix Scientific
Targets ......by Apexbio Technology LLC
Dasatinib, also known as?BMS-354825,?is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stri ......by BOC Sciences
Dasatinib is a multi-kinase inhibitor with potent activity against BCR–ABL kinase (IC₅₀ <1 nM) and Src family kinases (IC₅₀ = 0.2–1.1 nM). Dasatinib also inhibits Lyn (IC₅₀ = 8.5 nM) and Src (IC₅₀ = 3.0 nM) kinase activities in vitro using 0.1 mg/mL poly (Glu4-Tyr) as the substrate. ......by BioVision, Inc.,
A 100 mM (25 mg in 512 µl) solution of Dasatinib (Cat. No. 1586-25) in anhydrous DMSO. ......by BioVision, Inc.,
Dasatinib is a potent and dual AblWT/Src inhibitor IC50 of 0.6 nM/0.8 nM respectively; also inhibits c-KitWT/c-KitD816V with IC50 of 79 nM/37 nM. ......by MedChemexpress Co., Ltd.
Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations. SRC-family protein-tyrosine kinases interact with variety of cell-surface receptors and participate in intracellular signal transduction pathways; tumorigenic forms can occur through altered regulation or expression of the endogenous protein and by way of virally-encoded kinase genes. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus) Shelf life: >2 years if stored properly Drug formulation: ......by MedKoo Biosciences, Inc.
A potent, orally bioavailable, dual Src/Abl kinase inhibitor with IC50 of 0.5, 0.4, 0.5 and <1 nM for Src, Lck, Yes and Bcr-Abl, respectively; exhibits two-log increased potency relative to imatinib and retains activity against 14 of 15 imatinib-resistant BCR-ABL mutants; prolongs survival of mice with BCR-ABL-driven disease and inhibits proliferation of BCR-ABL-positive bone marrow progenitor cells from patients with imatinib-sensitive and imatinib-resistant CML.Blood CancerApproved ......by ProbeChem
Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. ......by Selleck Chemicals LLC
Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Cell lines DU-145 and LNCaP cells
Conditions 100 nM, 6 hours for inhibiting FAK phosphorylation 24 hours for decreasing cell-to-cell contact
Method Dasatinib almost totally abolished the levels of p-FAK at Tyr576/577 in DU-145 cells, whereas p-FAK was not detected in LNCaP cells even though both cell lines expressed similar levels of total FAK protein. Treatment with 100 nmol/L dasatinib for 24 hours had no effect on cell viability and total cell numbers, although partial inhibition of cell proliferation due to G1 arrest was observed at 48 and 72 hours. Besides, there was a substantial loss of cell-to-cell contact in DU-145 cells. This effect may be related to the decrease in levels of p-FAK and p-p130CAS.
Source Apexbio Technology LLC
Cell lines Ba/F3 cell lines
Conditions ~32 nM; 72 hours
Method Ba/F3 cell lines are seeded in triplicate and incubated with escalating concentrations of Dasatinib for 72 hours. Proliferation is measured using a methanethiosulfonate-based viability assay. IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges are 0 nM to 32 nM (Dasatinib). The Dasatinib concentration range is extended to 200 nM for mutant T315I.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models Pdx1-Cre, Z/EGFP, LSL-Kras G12D/+, LSL-Trp53R172H/+ mice
Dosage Form Oral administration, 10 mg/kg, daily
Applications There was no significant difference in survival between the different treatment groups. The median survival of vehicle-treated animals was 131 days compared with 127 days and 130 days for animals treated with dasatinib from 6 weeks and 10 weeks of age, respectively. Analysis of tumor burden in the mice showed that all mice had invasive PDAC; however, the number of mice with metastases was reduced significantly in dasatinib-treated animals. The incidence of metastases was 61.1% in vehicle-treated animals compared with 26.7% in mice treated with dasatinib from 6 weeks and 23.1% in mice treated with dasatinib from 10 weeks.
Source Apexbio Technology LLC
Animal Models EμLMP2A (TgE and Tg6 strains), MYC (λ-MYC), and LMP2A/λ-MYC double transgenic mice (Tg6/λ-MYC)
Dosage 30 mg/kg
Formulation DMSO
Administration Administered via i.p.
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000029066

Storage condition

Up to one week at 4°C or six months at -20°C. by Affix Scientific
Store at -20°C by Apexbio Technology LLC
Store at or below -20 oC. by LC Laboratoies

Solubility

Soluble in DMSO > 10 mM by Apexbio Technology LLC
Soluble in DMSO at 200 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10 μM; buffers, serum, or other additives may increase or decrease the aqueous solubility. by LC Laboratoies
DMSO ≥95mg/mL Water <1.2mg/mL Ethanol ≥3.8mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 98 mg/mL (200.81 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM); In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O5mg/mL by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Dasatinib Bristol-Myers Squibb Co Chronic myelocytic leukemia 2012/12/31 2014/9/30 Phase 4 Clinical
Dasatinib University of Newcastle Chronic myelocytic leukemia 2008/8/31 2017/8/31 Phase 3 Clinical
Dasatinib St Jude Children's Research Hospital Acute lymphoblastic leukemia 2007/10/31 2019/11/30 Phase 3 Clinical
Dasatinib Acute lymphoblastic leukemia 2008/7/31 2015/9/30 Phase 3 Clinical
Dasatinib - Launched
7

Safety Data of Dasatinib

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD37() USA
AbMole BioScience USA
Adipogen Corporation USA
AdooQ BioScience, LLC USA
Affix Scientific 500mg/USD955(In stock) USA
Apexbio Technology LLC USA
BOC Sciences
BioVision, Inc., USA
BioVision, Inc., USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 100mg/USD66();200mg/USD78() USA
Cayman Chemical Company USA
China Jintai Biocompound Company China
Gihi Chemicals Co., Ltd. China
Jintan Yufan Medicine Raw Materials Co., Ltd. China
LC Laboratoies 500mg/USD42(In stock);1g/USD57(In stock);2g/USD98(In stock);5g/USD172(In stock);10g/USD278(In stock);25g/USD690(In stock) USA
MedChemexpress Co., Ltd. 100mg/USD66();200mg/USD78() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Pure Chemistry Scientific Inc. 1g/USD65(In stock) USA
Selleck Chemicals LLC 10mM/1mLIn DMSO/USD140(In stock);25mg/USD147(In stock);100mg/USD370(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 100mg/USD66();200mg/USD78() China
Taizhou Huading Chemical Industry Co., Ltd. China
Target Molecule Corp. 5mg/USD52();10mg/USD83();50mg/USD133() USA
Wuxi Forest Biological Co., Ltd. China
Zhejiang Wonderful Pharma & Chem Co., Ltd. China
10

Related Products

Other Forms of 302962-49-8

Name CAS No Formula MW
Dasatinib (hydrochloride) 854001-07-3 C22H27Cl2N7O2S 524.47
Tazanolast 82989-25-1 C13H15N5O3 289.2899
Dasatinib (Monohydrate) 863127-77-9 C22H28ClN7O3S 506.0208
Dasatinib (D8) 1132093-70-9 C22H18D8ClN7O2S 496.05
Antibacterial compound 1 232951-56-3 C14H16FN3O4 309.29
PNU288034 383199-88-0 C16H19F2N3O5S 403.4
Spirendolol 81840-58-6 C21H31NO3 345.48
Taclamine 34061-33-1 C21H23N 289.41
Lidanserin 73725-85-6 C26H31FN2O4 454.53
RPR 238677 439278-74-7 C28H34FN7O3 535.61
Laflunimus 147076-36-6 C15H13F3N2O2 310.27
Terbufibrol 56488-59-6 C20H24O5 344.4
LAS-31180 137338-43-3 C11H12N2O3S 252.29

Recommended Compounds in Src Bcr-Abl Autophagy

Name CAS No Formula MW
Scutellarein 529-53-3 C15H10O6 286.24
A 419259 (trihydrochloride) 1435934-25-0 C29H37Cl3N6O 592.0
A 419259 364042-47-7 C29H34N6O 482.62
1-Naphthyl PP1 221243-82-9 C19H19N5 317.39
XL228 898280-07-4 C22H31N9O 437.54
Dasatinib (hydrochloride) 854001-07-3 C22H27Cl2N7O2S 524.47
MNS 1485-00-3 C9H7NO4 193.15618
PP2 172889-27-9 C15H16ClN5 301.77
PP1 172889-26-8 C16H19N5 281.36
ZM 306416 690206-97-4 C16H13ClFN3O2 333.74
AMG-47a 882663-88-9 C29H28F3N5O2 535.56
KX1-004 518058-84-9 C16H13FN2O2 284.29
AZM475271 476159-98-5 C23H27ClN4O3 442.9385
DCC-2036 1020172-07-9 C30H28FN7O3 553.59
Lck Inhibitor 847950-09-8 C31H30N8O 530.62
Lck inhibitor 2 944795-06-6 C18H17N5O2 335.36
PD173955 260415-63-2 C21H16Cl2N4OS 443.35
TG 100801 (Hydrochloride) 1018069-81-2 C33H31Cl2N5O3 616.54
TG 100801 867331-82-6 C33H30ClN5O3 580.08
TG 100572 (Hydrochloride) 867331-64-4 C26H27Cl2N5O2 512.43

Recommended Compounds in Same Indication

Name CAS No Formula MW
Panobinostat 404950-80-7 C21H23N3O2 349.43
Dexamethasone 50-02-2 C22H29FO5 392.46
Nordihydroguaiaretic acid 500-38-9 C18H22O4 302.36
Cyclophosphamide 50-18-0 C7H15Cl2N2O2P 261.09
Nilotinib 641571-10-0 C28H22F3N7O 529.52
Imatinib (hydrochloride) 862366-25-4 C29H32ClN7O 530.06
Imatinib (Mesylate) 220127-57-1 C30H35N7O4S 589.71
Dasatinib (hydrochloride) 854001-07-3 C22H27Cl2N7O2S 524.47
6-Mercaptopurine 50-44-2 C5H4N4S 152.18
Danusertib 827318-97-8 C26H30N6O3 474.55
Bosutinib 380843-75-4 C26H29Cl2N5O3 530.45
Lonafarnib 193275-84-2 C27H31Br2ClN4O2 638.82
Daunorubicin (Hydrochloride) 23541-50-6 C27H30ClNO10 563.98
PHA-680632 398493-79-3 C28H35N7O2 501.62
LDE225 (Diphosphate) 1218778-77-8 C26H32F3N3O11P2 681.49
Dexrazoxane (Hydrochloride) 149003-01-0 C11H17ClN4O4 304.73
Imatinib (Mesylate) 220127-57-1 C30H35N7O4S 589.7084
BMS-833923 1059734-66-5 C30H27N5O 473.57
Vinblastine (sulfate) 143-67-9 C46H60N4O13S 909.05
DCC-2036 1020172-07-9 C30H28FN7O3 553.59
11

Route of Synthesis

12

References

13

More Information

Dasatinib

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