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MedKoo Cat#: 100230 | Name: Dasatinib monohydrate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Dasatinib monohydrate
Dasatinib monohydrate
CAS#863127-77-9 (hydrate)

Theoretical Analysis

MedKoo Cat#: 100230

Name: Dasatinib monohydrate

CAS#: 863127-77-9 (hydrate)

Chemical Formula: C22H28ClN7O3S

Exact Mass: 487.1557

Molecular Weight: 506.02

Elemental Analysis: C, 52.22; H, 5.58; Cl, 7.01; N, 19.38; O, 9.49; S, 6.34

Price and Availability

Size Price Availability Quantity
200mg USD 150.00 Ready to ship
500mg USD 250.00 Ready to ship
1g USD 450.00 Ready to ship
2g USD 750.00 Ready to ship
5g USD 1,450.00 Ready to Ship
10g USD 2,450.00 Ready to Ship
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Related CAS #
863127-77-9 (hydrate) 302962-49-8 (free) 2112837-79-1 (cabaldehyde) 910297-52-8 (N-oxide)
Synonym
BMS-354825; BMS 354825; BMS354825; Dasatinib; US brand name: Sprycel.
IUPAC/Chemical Name
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide monohydrate.
InChi Key
XHXFZZNHDVTMLI-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H26ClN7O2S.H2O/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);1H2
SMILES Code
O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCO)CC3)=C2)S1)NC4=C(C)C=CC=C4Cl.[H]O[H]
Appearance
white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# 863127-77-9 (Dasatinib monohydrate); 302962-49-8 (Dasatinib).
Biological target:
Dasatinib (BMS-354825) monohydrate is an inhibitor that targets Abl, Src and c-Kit with IC50s of <1 nM, 0.8 nM and 79 nM, respectively.
In vitro activity:
Dasatinib inhibited tyrosine kinase and induced eryptosis in human erythrocytes with early denature of esterase, cell shrinkage, loss of membrane integrity with inside-out phosphatidylserine, increase in the cytosolic Ca2+ ion concentration ([Ca2+]i), caspase-3 activation and change in cellular redox state. Mechanistically, the rise of [Ca2+]i seems to be a key mediator in the dasatinib-mediated eryptosis because depletion of external Ca2+ could suppress the eryptotic effects. Also, dasatinib was able to reduce membrane fluidity in human RBCs. For the direct action on membrane, dasatinib permeabilized RBC ghosts in a way similar to digitonin. Dasatinib inhibited tyrosine kinase and induced eryptosis in human erythrocytes through Ca2+ loading and membrane permeabilization. Reference: Toxicol Lett. 2018 Oct 1;295:10-21. https://www.sciencedirect.com/science/article/abs/pii/S0378427418302273?via%3Dihub
In vivo activity:
In vivo effects of Dasatinib treatment on the occurrence of skeletal metastases were tested in a xenograft mouse model after intra-cardiac injection of osteotropic MDA-MB-231-cells. Mice which received an intra-peritoneal treatment with Dasatinib showed significantly less skeletal metastases in bioluminescence scans. Moreover, a pronounced increase in bone volume was observed in the treatment group, as detected by µ-Computed Tomography. Dasatinib treatment also led to a greater increase in bone density in tibiae without metastatic affection, which was accompanied by reduced recruitment of osteoclasts. Reference: Arch Gynecol Obstet. 2020 Jun;301(6):1493-1502. https://link.springer.com/article/10.1007%2Fs00404-020-05496-4
Solvent mg/mL mM
Solubility
DMSO 100.0 197.62
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 506.02 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Sheng LX, Wang JP, Lai YL, Wu H, Sun YC, Zhou M, Ouyang GF, Huang H. [Effects of Dasatinib on the Expansion, Subsets, Receptor Expression and Cytotoxic Function of NK Cells in Vitro]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2020 Oct;28(5):1762-1768. Chinese. doi: 10.19746/j.cnki.issn.1009-2137.2020.05.055. PMID: 33067987. 2. Chan WY, Lau PM, Yeung KW, Kong SK. The second generation tyrosine kinase inhibitor dasatinib induced eryptosis in human erythrocytes-An in vitro study. Toxicol Lett. 2018 Oct 1;295:10-21. doi: 10.1016/j.toxlet.2018.05.030. Epub 2018 May 24. PMID: 29803841. 3. Abdelgalil AA, Alam MA, Raish M, Mohammed IE, Hassan Mohammed AE, Ansari MA, Al Jenoobi FI. Dasatinib significantly reduced in vivo exposure to cyclosporine in a rat model: The possible involvement of CYP3A induction. Pharmacol Rep. 2019 Apr;71(2):201-205. doi: 10.1016/j.pharep.2018.10.018. Epub 2018 Oct 31. PMID: 30785057. 4. Heilmann T, Rumpf AL, Roscher M, Tietgen M, Will O, Gerle M, Damm T, Borzikowsky C, Maass N, Glüer CC, Tiwari S, Trauzold A, Schem C. Dasatinib prevents skeletal metastasis of osteotropic MDA-MB-231 cells in a xenograft mouse model. Arch Gynecol Obstet. 2020 Jun;301(6):1493-1502. doi: 10.1007/s00404-020-05496-4. Epub 2020 Mar 14. PMID: 32170411.
In vitro protocol:
1. Sheng LX, Wang JP, Lai YL, Wu H, Sun YC, Zhou M, Ouyang GF, Huang H. [Effects of Dasatinib on the Expansion, Subsets, Receptor Expression and Cytotoxic Function of NK Cells in Vitro]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2020 Oct;28(5):1762-1768. Chinese. doi: 10.19746/j.cnki.issn.1009-2137.2020.05.055. PMID: 33067987. 2. Chan WY, Lau PM, Yeung KW, Kong SK. The second generation tyrosine kinase inhibitor dasatinib induced eryptosis in human erythrocytes-An in vitro study. Toxicol Lett. 2018 Oct 1;295:10-21. doi: 10.1016/j.toxlet.2018.05.030. Epub 2018 May 24. PMID: 29803841.
In vivo protocol:
1. Abdelgalil AA, Alam MA, Raish M, Mohammed IE, Hassan Mohammed AE, Ansari MA, Al Jenoobi FI. Dasatinib significantly reduced in vivo exposure to cyclosporine in a rat model: The possible involvement of CYP3A induction. Pharmacol Rep. 2019 Apr;71(2):201-205. doi: 10.1016/j.pharep.2018.10.018. Epub 2018 Oct 31. PMID: 30785057. 2. Heilmann T, Rumpf AL, Roscher M, Tietgen M, Will O, Gerle M, Damm T, Borzikowsky C, Maass N, Glüer CC, Tiwari S, Trauzold A, Schem C. Dasatinib prevents skeletal metastasis of osteotropic MDA-MB-231 cells in a xenograft mouse model. Arch Gynecol Obstet. 2020 Jun;301(6):1493-1502. doi: 10.1007/s00404-020-05496-4. Epub 2020 Mar 14. PMID: 32170411.
1: Lindauer M, Hochhaus A. Dasatinib. Recent Results Cancer Res. 2018;212:29-68. doi: 10.1007/978-3-319-91439-8_2. PMID: 30069624. 2: Hořínková J, Šíma M, Slanař O. Pharmacokinetics of Dasatinib. Prague Med Rep. 2019;120(2-3):52-63. doi: 10.14712/23362936.2019.10. PMID: 31586504. 3: Cortes JE, Jimenez CA, Mauro MJ, Geyer A, Pinilla-Ibarz J, Smith BD. Pleural Effusion in Dasatinib-Treated Patients With Chronic Myeloid Leukemia in Chronic Phase: Identification and Management. Clin Lymphoma Myeloma Leuk. 2017 Feb;17(2):78-82. doi: 10.1016/j.clml.2016.09.012. Epub 2016 Sep 17. PMID: 28082112. 4: Ryu KY, Lee HJ, Woo H, Kang RJ, Han KM, Park H, Lee SM, Lee JY, Jeong YJ, Nam HW, Nam Y, Hoe HS. Dasatinib regulates LPS-induced microglial and astrocytic neuroinflammatory responses by inhibiting AKT/STAT3 signaling. J Neuroinflammation. 2019 Oct 26;16(1):190. doi: 10.1186/s12974-019-1561-x. PMID: 31655606; PMCID: PMC6815018. 5: Levêque D, Becker G, Bilger K, Natarajan-Amé S. Clinical Pharmacokinetics and Pharmacodynamics of Dasatinib. Clin Pharmacokinet. 2020 Jul;59(7):849-856. doi: 10.1007/s40262-020-00872-4. PMID: 32112275. 6: Hickson LJ, Langhi Prata LGP, Bobart SA, Evans TK, Giorgadze N, Hashmi SK, Herrmann SM, Jensen MD, Jia Q, Jordan KL, Kellogg TA, Khosla S, Koerber DM, Lagnado AB, Lawson DK, LeBrasseur NK, Lerman LO, McDonald KM, McKenzie TJ, Passos JF, Pignolo RJ, Pirtskhalava T, Saadiq IM, Schaefer KK, Textor SC, Victorelli SG, Volkman TL, Xue A, Wentworth MA, Wissler Gerdes EO, Zhu Y, Tchkonia T, Kirkland JL. Senolytics decrease senescent cells in humans: Preliminary report from a clinical trial of Dasatinib plus Quercetin in individuals with diabetic kidney disease. EBioMedicine. 2019 Sep;47:446-456. doi: 10.1016/j.ebiom.2019.08.069. Epub 2019 Sep 18. Erratum in: EBioMedicine. 2020 Feb;52:102595. PMID: 31542391; PMCID: PMC6796530. 7: Rousselot P, Coudé MM, Gokbuget N, Gambacorti Passerini C, Hayette S, Cayuela JM, Huguet F, Leguay T, Chevallier P, Salanoubat C, Bonmati C, Alexis M, Hunault M, Glaisner S, Agape P, Berthou C, Jourdan E, Fernandes J, Sutton L, Banos A, Reman O, Lioure B, Thomas X, Ifrah N, Lafage-Pochitaloff M, Bornand A, Morisset L, Robin V, Pfeifer H, Delannoy A, Ribera J, Bassan R, Delord M, Hoelzer D, Dombret H, Ottmann OG; European Working Group on Adult ALL (EWALL) group. Dasatinib and low-intensity chemotherapy in elderly patients with Philadelphia chromosome-positive ALL. Blood. 2016 Aug 11;128(6):774-82. doi: 10.1182/blood-2016-02-700153. Epub 2016 Apr 27. PMID: 27121472; PMCID: PMC5085255. 8: Cortes JE, Saglio G, Kantarjian HM, Baccarani M, Mayer J, Boqué C, Shah NP, Chuah C, Casanova L, Bradley-Garelik B, Manos G, Hochhaus A. Final 5-Year Study Results of DASISION: The Dasatinib Versus Imatinib Study in Treatment-Naïve Chronic Myeloid Leukemia Patients Trial. J Clin Oncol. 2016 Jul 10;34(20):2333-40. doi: 10.1200/JCO.2015.64.8899. Epub 2016 May 23. PMID: 27217448; PMCID: PMC5118045. 9: Saccon TD, Nagpal R, Yadav H, Cavalcante MB, Nunes ADC, Schneider A, Gesing A, Hughes B, Yousefzadeh M, Tchkonia T, Kirkland JL, Niedernhofer LJ, Robbins PD, Masternak MM. Senolytic Combination of Dasatinib and Quercetin Alleviates Intestinal Senescence and Inflammation and Modulates the Gut Microbiome in Aged Mice. J Gerontol A Biol Sci Med Sci. 2021 Oct 13;76(11):1895-1905. doi: 10.1093/gerona/glab002. PMID: 33406219; PMCID: PMC8514064. 10: Sugiura I, Doki N, Hata T, Cho R, Ito T, Suehiro Y, Tanaka M, Kako S, Matsuda M, Yokoyama H, Ishikawa Y, Taniguchi Y, Hagihara M, Ozawa Y, Ueda Y, Hirano D, Sakura T, Tsuji M, Kamae T, Fujita H, Hiramoto N, Onoda M, Fujisawa S, Hatta Y, Dobashi N, Nishiwaki S, Atsuta Y, Kobayashi Y, Hayakawa F, Ohtake S, Naoe T, Miyazaki Y. Dasatinib-based 2-step induction for adults with Philadelphia chromosome-positive acute lymphoblastic leukemia. Blood Adv. 2022 Jan 25;6(2):624-636. doi: 10.1182/bloodadvances.2021004607. PMID: 34516628; PMCID: PMC8791587. 11: Alqattan Y, Ali S, Almohammad R, Kayali N, Alhuraiji A. Dasatinib-induced Chylothorax in Chronic Myeloid Leukemia. Gulf J Oncolog. 2022 Sep;1(40):74-77. PMID: 36448074. 12: Advani AS, Moseley A, O'Dwyer KM, Wood BL, Park J, Wieduwilt M, Jeyakumar D, Yaghmour G, Atallah EL, Gerds AT, O'Brien SM, Liesveld JL, Othus M, Litzow M, Stone RM, Sharon E, Erba HP. Dasatinib/prednisone induction followed by blinatumomab/dasatinib in Ph+ acute lymphoblastic leukemia. Blood Adv. 2023 Apr 11;7(7):1279-1285. doi: 10.1182/bloodadvances.2022008216. PMID: 36322825; PMCID: PMC10090098. 13: Özgür Yurttaş N, Eşkazan AE. Dasatinib-induced pulmonary arterial hypertension. Br J Clin Pharmacol. 2018 May;84(5):835-845. doi: 10.1111/bcp.13508. Epub 2018 Mar 6. PMID: 29334406; PMCID: PMC5903230. 14: Tamura Y, Tamura Y. Dasatinib-induced Pulmonary Hypertension. Intern Med. 2022 Aug 1;61(15):2245-2246. doi: 10.2169/internalmedicine.9107-21. Epub 2022 Feb 1. PMID: 35110497; PMCID: PMC9424095. 15: Fauziya, Gupta A, Nadaf A, Ahmad S, Hasan N, Imran M, Sahebkar A, Jain GK, Kesharwani P, Ahmad FJ. Dasatinib: a potential tyrosine kinase inhibitor to fight against multiple cancer malignancies. Med Oncol. 2023 May 10;40(6):173. doi: 10.1007/s12032-023-02018-5. PMID: 37165283. 16: Islam MT, Tuday E, Allen S, Kim J, Trott DW, Holland WL, Donato AJ, Lesniewski LA. Senolytic drugs, dasatinib and quercetin, attenuate adipose tissue inflammation, and ameliorate metabolic function in old age. Aging Cell. 2023 Feb;22(2):e13767. doi: 10.1111/acel.13767. Epub 2023 Jan 13. PMID: 36637079; PMCID: PMC9924942. 17: Miura M. Therapeutic drug monitoring of imatinib, nilotinib, and dasatinib for patients with chronic myeloid leukemia. Biol Pharm Bull. 2015;38(5):645-54. doi: 10.1248/bpb.b15-00103. PMID: 25947908. 18: Brattås MK, Reikvam H, Tvedt THA, Bruserud Ø. Dasatinib as an investigational drug for the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia in adults. Expert Opin Investig Drugs. 2019 May;28(5):411-420. doi: 10.1080/13543784.2019.1597052. Epub 2019 Apr 5. PMID: 30916583. 19: Barkoulas T, Hall PD. Experience with dasatinib and nilotinib use in pregnancy. J Oncol Pharm Pract. 2018 Mar;24(2):121-128. doi: 10.1177/1078155217692399. Epub 2017 Feb 17. PMID: 29284357. 20: McCafferty EH, Dhillon S, Deeks ED. Dasatinib: A Review in Pediatric Chronic Myeloid Leukemia. Paediatr Drugs. 2018 Dec;20(6):593-600. doi: 10.1007/s40272-018-0319-8. PMID: 30465234.