Dasatinib

 CAS No.: 302962-49-8  Cat No.: BP-300077  Purity: >98%  HPLC  HNMR  MS 4.5  

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 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.

Dasatinib

Structure of 302962-49-8

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Ligand for Target Protein
Molecular Formula
C22H26ClN7O2S
Molecular Weight
488.01
Appearance
White to Off-White Solid

* For research and manufacturing use only. Not for human or clinical use.

SizePriceStockQuantity
25 g $489 In stock

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Purity
>98%
Appearance
White to Off-White Solid
Synonyms
BMS-354825; BMS354825; BMS354825
Melting Point
>250°C (dec.)
InChI Key
ZBNZXTGUTAYRHI-UHFFFAOYSA-N
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)
Canonical SMILES
CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=NC(=NC(=C3)N4CCN(CC4)CCO)C
1.Successful pregnancy involving a man with chronic myeloid leukemia on dasatinib
Houssam Oweini • Zaher K. Otrock. Arch Gynecol Obstet (2011) 283:133–134
On January 2008, dasatinib (70 mg twice daily) was started. The patient tolerated treatment well with no significant side effects. He was being followed up regularly with blood studies. By the end of February 2009 he informed us that his wife had a successful delivery of a healthy baby boy after a full term pregnancy. The baby was 3.1 kg and 46 cm with no congenital anomalies. At the time of conception, the patient was receiving dasatinib 140 mg/day, and the cumulative dose of dasatinib was approximated 350 g. At the time of writing this report, the patient was doing well on dasatinib. His last evaluation showed that he was in complete hematological response with no molecular response (quantitative analysis of peripheral blood BCR-ABL mRNA levels using real-time polymerase chain reaction were 6.00E-2, relative expression ratio of bcr-abl to G6PDH (ROCHE Diagnostics, Light Cycler 2.0). His baby was 7 months old, and he was in good health.
2.H2-receptor antagonist influences dasatinib pharmacokinetics in a patient with Philadelphia-positive acute lymphoblastic leukemia
Akihito Matsuoka • Naoto Takahashi • Masatomo Miura • Takenori Niiok. Cancer Chemother Pharmacol (2012) 70:351–352
Takahashi et al. recently reported in this journal that administration of an acid suppressant such as an H2-receptor antagonist (H2RA) and a proton pump inhibitor can decrease the absorption of dasatinib from the gastrointestinal tract, thereby resulting in a significant decrease in plasma dasatinib concentration. Here, we report a patient treated with dasatinib and H2RA famotidine whose plasma dasatinib concentration increased dramatically after the cessation of famotidine.
ConcentrationVolumeMass1 mg5 mg10 mg
1 mM2.0491 mL10.2457 mL20.4914 mL
5 mM0.4098 mL2.0491 mL4.0983 mL
10 mM0.2049 mL1.0246 mL2.0491 mL
50 mM0.0410 mL0.2049 mL0.4098 mL

I want to purchase Dasatinib. And how does Dasatinib cause keratinocyte apoptosis?

Dasatinib causes keratinocyte apoptosis via inhibiting high mobility group Box 1-mediated mitophagy.

31/7/2016

Dear Sir, please give information about how Dasatinib ameliorates chronic pancreatitis induced by caerulein.

Dasatinib ameliorates chronic pancreatitis induced by caerulein via anti-fibrotic and anti-inflammatory mechanism.

28/11/2017

Dear Sir, please give information about how Dasatinib protects against acute respiratory distress syndrome?

Dasatinib protects against acute respiratory distress syndrome via Nrf2-regulated M2 macrophages polarization.

18/2/2021

show anti-proliferative activity in human prostate tumor

Compared with K562 CML and PC3, Dasatinib showed great anti-proliferative activity in human prostate tumor, MDA-MB-231 human breast tumor and WiDr human colon tumor cell lines with IC50 of 1.0 nM, 9.4 nM, 12 nM and 52 nM, respectively. Worked perfectly.

9/12/2018

antitumor activity

In my project, Dasatinib has potent antitumor activity and a high margin of safety in a K562 xenograft model of chronic myelogenous leukemia (CML), indicating complete tumor regression and low multi-dose level toxicity. It worked well in our experiments, happy with purchase.

9/9/2022

have significant activity on Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1 and MEK

In my study, Dasatinib has significant activity on Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1 and MEK, with IC50 of 1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively. Great performance.

9/12/2022

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* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2

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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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