ACP196 is , while it's Molecular Formula is C26H23N7O2. Acalabrutinib, is an experimental anti-cancer drug and a selective Bruton's tyrosine kinase (BTK) inhibitor. This kinase transmits signals from B-cell Receptor (BCR), and thus any genetic BTK mutation causes B-Cell immunodeficiency. Therefore, BTK inhibitors targeting B-cell signaling has shown great promise for the treatment of chronic lymphocytic leukemia (CLL).

What is the CAS number for ACP196?

The CAS number of ACP196 is 1420477-60-6.

What is ACP196 (1420477-60-6) used for?

Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 3 nM, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR.

ACP196 is , while it's Molecular Formula is C26H23N7O2. Acalabrutinib, is an experimental anti-cancer drug and a selective Bruton's tyrosine kinase (BTK) inhibitor. This kinase transmits signals from B-cell Receptor (BCR), and thus any genetic BTK mutation causes B-Cell immunodeficiency. Therefore, BTK inhibitors targeting B-cell signaling has shown great promise for the treatment of chronic lymphocytic leukemia (CLL).

What is the CAS number for ACP196?

The CAS number of ACP196 is 1420477-60-6.

What is ACP196 (1420477-60-6) used for?

Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 3 nM, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR.

Product Class

1420477-60-6

Product Name：Acalabrutinib
Molecular Formula：C26H23N7O2
Purity：99%
Molecular Weight：465.514

Inquiry

Product Details:

CasNo： 1420477-60-6

Molecular Formula： C26H23N7O2

Buy High Grade 1420477-60-6 Fast Shipping, Export Acalabrutinib

Molecular Formula:C26H23N7O2
Molecular Weight:465.514
PKA:11.47±0.70(Predicted)
PSA：118.51000
Density:1.37±0.1 g/cm3(Predicted)
LogP:3.90470

Acalabrutinib(Cas 1420477-60-6) Usage

Description

Acalabrutinib, marketed as Calquence, is a medication utilized for the treatment of various non-Hodgkin lymphomas, specifically mantle cell lymphoma and chronic lymphocytic leukemia/small lymphocytic lymphoma. This tyrosine kinase inhibitor (TKI) is employed in both relapsed and treatment-naive scenarios. Calquence (acalabrutinib) is a drug used to treat patients with blood cancers, including chronic lymphocytic leukemia or small lymphocytic lymphoma (CLL/SLL) and mantle cell lymphoma (MCL) that does not respond to other treatments or returns following initial treatment response.

Uses

Acalabrutinib, classified as a chemotherapy and antineoplastic drug, operates by inhibiting the enzyme tyrosine kinase, impeding cell growth and division. In clinical studies like ASCEND and ELEVATE, acalabrutinib monotherapy and its combination with obinutuzumab exhibited enhanced efficacy and a well-tolerated safety profile, establishing its effectiveness and safety in the treatment of chronic lymphocytic leukemia. Acalabrutinib works by blocking Bruton's tyrosine kinase (BTK) signaling. This helps stop cancerous B cells from surviving and multiplying, which may slow the spread of cancer. This trial also checks for MRD after treatment with obinutuzumab and venetoclax. On November 21, 2019, the U.S. Food and Drug Administration (FDA) announced it has approved the use of acalabrutinib (CALQUENCE, AstraZeneca) as a monotherapy for the treatment of chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL).

1420477-60-6 Relevant articles

Acalabrutinib in relapsed or refractory mantle cell lymphoma (ACE-LY-004): a single-arm, multicentre, phase 2 trial

Prof Michael Wang, MDa,b miwang@mdanderson.org ∙ Prof Simon Rule, MDc ∙ Prof Pier Luigi Zinzani, MDd ∙ Prof Andre Goy, MDe ∙ Prof Olivier Casasnovas, MDf ∙ Stephen D Smith, MDg

, The Lancet, Volume 391, Issue 10121p659-667February 17, 2018

In this open-label, phase 2 study, oral acalabrutinib (100 mg twice per day) was given to patients with relapsed or refractory mantle cell lymphoma, until disease progression or unacceptable toxicity. The primary endpoint was overall response assessed according to the Lugano classification, and safety analyses were done in all participants.

Resistance to Acalabrutinib in CLL Is Mediated Primarily By BTK Mutations

Jennifer Woyach MD 1, Ying Huang MS, MA * 2, Kerry Rogers * 2, Seema A. Bhat MD 2, Michael R. Grever MD 2, Arletta Lozanski * 2, Tzyy-Jye Doong * 2, James S. Blachly MD 2, Gerard Lozanski MD 2, Dan Jones MD PhD 2, John C. Byrd MD 3

, Blood, Volume 134, Supplement 1, 13 November 2019, Page 504

All patients (pts) treated at The Ohio State University and enrolled on an IRB approved phase 1b/2 study in CLL were included in this analysis. Beginning 12 months (mos) after the initiation of Acalabrutinib, pts underwent deep sequencing every 3-6 cycles using a digital droplet PCR assay for BTK C481S or Ion Torrent Sequencing for any BTK or PLCG2 mutations.

1420477-60-6 Process route

: 590-93-2
2-Butynoic acid

: 1420478-90-5
4-{8-amino-3-[(2S)-pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)benzamide

: 1420477-60-6,1952316-43-6
4-{8-amino-3-[(2S)-1-(1-oxo-2-butyn-1-yl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)benzamide

Conditions

Conditions	Yield
With triethylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; In dichloromethane; at 20 - 30 ℃; for 3h;	90%
With 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide; triethylamine; In dichloromethane; Large scale;	74%
With 1-hydroxy-pyrrolidine-2,5-dione; dicyclohexyl-carbodiimide; In dichloromethane; at -15 - 5 ℃; for 3h; Reagent/catalyst;	72%
With triethylamine; HATU; In dichloromethane; at 20 ℃; for 0.5h;	18%
With triethylamine; HATU; In dichloromethane; at 20 ℃; for 0.5h;	18%
With triethylamine; HATU; In dichloromethane; at 20 ℃; for 0.5h;	18%
With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; In dichloromethane; at 20 ℃; Reagent/catalyst;	219 g
With triethylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; In dichloromethane; at 20 ℃; for 2h;	9.2 g
With triethylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate; In dichloromethane; at 20 ℃; for 2h;	9.2 g
2-Butynoic acid; With 1H-imidazole; In dichloromethane; at 0 - 30 ℃; for 0.666667h; With pivaloyl chloride; In dichloromethane; at 0 - 0.1 ℃; for 1.08333h; 4-{8-amino-3-[(2S)-pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)benzamide; In dichloromethane; for 0.5h;

: 4-[8-chloro-3-[(2S)-1-(1-oxo-2-butyn-1-yl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridylbenzamide

: 1420477-60-6,1952316-43-6
4-{8-amino-3-[(2S)-1-(1-oxo-2-butyn-1-yl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)benzamide