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Dasatinib monohydrate

Dasatinib monohydrate structure

CAS No:
863127-77-9
Formula:
C22H26ClN7O2S.H2O
Chemical Name:
Dasatinib monohydrate
Synonyms:
5-Thiazolecarboxamide,N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-,hydrate (1:1);5-Thiazolecarboxamide,N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-,monohydrate;BMS 35482503;Dasatinib hydrate;Dasatinib monohydrate
Categories:
Active Pharmaceutical Ingredients > Antineoplastic Agents

Description

ChEBI: A hydrate that is the monohydrate of dasatinib. It is used for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhyd ous dasatinib (INN).

Dasatinib monohydrate is a hydrate that is the monohydrate of dasatinib. It is used for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). It has a role as an antineoplastic agent and a tyrosine kinase inhibitor. It contains a dasatinib (anhydrous).|Dasatinib is a selective tyrosine kinase receptor inhibitor that is used in the therapy of chronic myelogenous leukemia (CML) positive for the Philadelphia chromosome. Dasatinib is commonly associated with transient elevations in serum aminotransferase levels during treatment, but with only rare instances of clinically apparent acute liver injury.|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 a 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.|A pyrimidine and thiazole derived ANTINEOPLASTIC AGENT and PROTEIN KINASE INHIBITOR of BCR-ABL KINASE. It is used in the treatment of patients with CHRONIC MYELOID LEUKEMIA who are resistant or intolerant to IMATINIB.

Dasatinib monohydrate Basic Attributes

Molecular Weight：

506.02082

Exact Mass：

505.166

UNII：

RBZ1571X5H

DSSTox ID：

DTXSID50235486

NCI Thesaurus Code：

C38713

HScode：

29339900

Characteristics

PSA：

136

XLogP3：

3.39810

Density：

1.408 g/cm3

Melting Point：

97-99 °C(lit.)

Safety Information

Packing level：

Hazard category：

4.3

Transport codes：

UN 3263 8/PG 2

wgk germany：

hazard class code：

R34; R36/37/38

safety instructions：

S26; S27; S28

RTECS Number：

QD8530000

Marks：

C; Xi

Precautionary statement(s)：

P201, P202, P260, P263, P264, P270, P273, P281, P301+P310, P308+P313, P309+P311, P314, P321, P330, P391, P405, P501

Hazard Statements：

H300

GHS Classification：

|Danger|H300 (75%): Fatal if swallowed [Danger Acute toxicity, oral]|P201, P202, P260, P263, P264, P270, P273, P281, P301+P310, P308+P313, P309+P311, P314, P321, P330, P391, P405, and P501|Aggregated GHS information provided by 4 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Hepatotoxicity：

In large clinical trials, elevations in serum aminotransferase levels during dasatinib therapy occurred in up to 50% of patients, but were usually mild and self-limited. Elevations above 5 times the upper limit of normal (ULN) occurred in 1% to 9% of patients and generally responded to dose adjustment or temporary discontinuation and restarting at a lower dose, which is recommended if liver test results are markedly elevated (ALT or AST persistently greater than 5 times ULN or bilirubin more than 3 times ULN). While episodes of marked serum aminotransferase elevations with symptoms have been reported, there have been no published reports of clinically apparent liver injury with jaundice attributed to dasatinib therapy. Certainly other tyrosine kinase receptor inhibitors used in the therapy of CML such as imatinib, nilotinib and ponatinib have been associated with cases of acute liver injury with jaundice. With these agents, the liver injury typically arises after several months of therapy and the pattern of serum enzyme elevations is typically hepatocellular. Immunoallergic features (rash, fever and eosinophilia) and autoantibody formation are usually not present.

Drug Information

LiverTox Summary：

Dasatinib is a selective tyrosine kinase receptor inhibitor that is used in the therapy of chronic myelogenous leukemia (CML) positive for the Philadelphia chromosome. Dasatinib is commonly associated with transient elevations in serum aminotransferase levels during treatment, but with only rare instances of clinically apparent acute liver injury.

Drug Classes：

Antineoplastic Agents

MeSH：

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)|Agents that inhibit PROTEIN KINASES. (See all compounds classified as Protein Kinase Inhibitors.)

MeSH Entry Terms：

(18F)-N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide

Dasatinib monohydrate Use and Manufacturing

antineoplastic

Computed Properties

Molecular Weight:506.0
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:10
Rotatable Bond Count:7
Exact Mass:505.1662866
Monoisotopic Mass:505.1662866
Topological Polar Surface Area:136
Heavy Atom Count:34
Complexity:642
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

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