131740-09-5|盐酸夫拉平度|Flavopiridol Hydrochloride|MFCD26792554-范德生物科技公司

盐酸夫拉平度

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names：
Flavopiridol Hydrochloride
CAS号：
131740-09-5
MDL Number： MFCD26792554
MF(分子式)： C21H21Cl2NO5 MW(分子量)： 438.3
EINECS:634-346-4 Reaxys Number:No data available
Pubchem ID:9910986 Brand:BIOFOUNT

盐酸夫拉平度Flavopiridol Hydrochloride(131740-09-5,HMR 1275,L 868275)与ATP竞争抑制CDK，包括CDK1，CDK2，CDK4和CDK6，IC50约为40 nM。对CDK1 / 2/4/6的选择性是CDK7的7.5倍。最初发现Flavopiridol可抑制EGFR和PKA。IC50值：40 nM；靶标：CDK；体外：Flavopiridol以时间和浓度依赖性方式抑制人乳腺癌细胞中的CDK2和CDK4诱导G1阻滞。Flavopiridol的短时治疗（约12小时）在造血细胞系中诱导凋亡，包括SUDHL4，SUDHL6（B细胞系），Jurkat和MOLT4（T细胞系）以及HL60（骨髓）。在克隆形成测定中，黄酮哌啶醇在23种人类肿瘤模型中起高效细胞毒性化合物的作用，平均IC70为8 ng / mL。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
HCR201070-10mg	10mg	97%	¥ 731.50	¥ 731.50		4-7周	- +	¥ 0.00

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中文别名	盐酸夫拉平度(131740-09-5),夫拉平度盐酸盐,盐酸氟哌啶醇,阿沃地比,黄酮哌啶醇,（-）顺式5,7-二羟基-2-（2-氯苯基）-8-（4-（3-羟基-1-甲基）哌啶基）-4H-1-苯并吡喃-4-酮;
英文别名	Flavopiridol Hydrochloride(131740-09-5);HMR 1275;L 868275;L-868275;L86-8275;alvocidib;flavopiridol;(-)cis-5,7-dihydroxy-2-(2-chlorophenyl)-8-(4-(3-hydroxy-1-methyl)piperidinyl)-4H-1-benzopyran-4-one;
CAS号	131740-09-5
Inchi	InChI=1S/C21H20ClNO5.ClH/c1-23-7-6-12(17(27)10-23)19-14(24)8-15(25)20-16(26)9-18(28-21(19)20)11-4-2-3-5-13(11)22;/h2-5,8-9,12,17,24-25,27H,6-7,10H2,1H3;1H/t12-,17+;/m0./s1
InchiKey	LGMSNQNWOCSPIK-LWHGMNCYSA-N
分子式 Formula	C21H21Cl2NO5
分子量 Molecular Weight	438.3
溶解度Solubility	生物体外In Vitro:H2O≥ 20 mg/mL(45.63 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性状	白色至浅棕色粉末
储藏条件 Storage conditions	2-8oC

盐酸夫拉平度,Flavopiridol Hydrochloride(131740-09-5,HMR 1275,L 868275)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染
Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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产品说明	盐酸夫拉平度Flavopiridol Hydrochloride(131740-09-5,HMR 1275,L 868275)是细胞周期蛋白依赖性激酶的抑制剂,抑制或阻止NEOPLASMS增殖的物质。
Introduction	盐酸夫拉平度Flavopiridol Hydrochloride(131740-09-5,HMR 1275,L 868275)is an inhibitor of cyclin-dependent kinases, which inhibits or prevents the proliferation of NEOPLASMS.
Application1	盐酸夫拉平度（Alvocidib Hydrochloride）是一种CDK的广谱抑制剂，与ATP竞争性地抑制CDK1，CDK2和CDK4的活性，IC50 值分别为30、170、100 nM。
Application2
Application3

盐酸夫拉平度,Flavopiridol Hydrochloride(131740-09-5,HMR 1275,L 868275)是一种合成的N-甲基哌啶基氯苯基黄酮化合物。作为细胞周期蛋白依赖性激酶的抑制剂，alvocidib通过阻止细胞周期蛋白依赖性激酶（CDK）的磷酸化和下调细胞周期蛋白D1和D3的表达来诱导细胞周期停滞，从而导致G1细胞周期停滞和凋亡。盐酸夫拉平度还是三磷酸腺苷活性的竞争性抑制剂。盐酸夫拉平度是生长抑制剂，抑制人类和动物细胞或微生物正常生长的内源性或外源性物质，不同于影响植物生长的物质（=植物生长调节剂）。盐酸夫拉平度是蛋白激酶抑制剂，抑制蛋白激酶的药物。抗肿瘤药抑制或阻止NEOPLASMS增殖的物质。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H333吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P313获得医疗建议/护理
备注	Flavopiridol Hydrochloride实验过程中防止吸入、食入，做好安全防护

盐酸夫拉平度,Flavopiridol Hydrochloride(131740-09-5,HMR 1275,L 868275)危害标识：

象形图
信号	Warning
GHS危险说明	Aggregated GHS information provided by 40 companies from 2 notifications to the ECHA C&L Inventory.
	H302 (95%): Harmful if swallowed [Warning Acute toxicity, oral]
	Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范说明代码	P264, P270, P301+P312, P330, and P501
防范说明代码	(The corresponding statement to each P-code can be found at the GHS Classification page.)

Mahoney E, et al. ER stress and autophagy: new discoveries in the mechanism of action and drug resistance of the cyclin-dependent kinase inhibitor flavopiridol.Blood. 2012 Aug 9;120(6):1262-1273.

Keskin H, et al. Complex effects of flavopiridol on the expression of primary response genes. Cell Div. 2012 Mar 29;7:11.

Kim KS, et al.Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects. J Med Chem. 2000 Nov 2;43(22):4126-34.

Flavopiridol (L86 8275; NSC 649890), a new kinase inhibitor for tumor therapy PMID 21541623; International journal of oncology 1996 Dec; 9(6):1143-68 Name matches: diarrhea nsc 649890

Gateways to clinical trials PMID 17136234; Methods and findings in experimental and clinical pharmacology 2006 Oct; 28(8):533-91 Name matches: human papillomavirus alvocidib hydrochloride

盐酸夫拉平度,Flavopiridol Hydrochloride(131740-09-5,HMR 1275,L 868275)参考文献：

1，Gateways to clinical trials.
Tomillero A1, Moral MA. Methods Find Exp Clin Pharmacol. 2008 Jun;30(5):383-408.
(+)-Dapoxetine hydrochloride, (R)-Etodolac; Abatacept, ABT-510, Adalimumab, Agatolimod sodium, Alemtuzumab, Alvocidib hydrochloride, Aminolevulinic acid methyl ester, Aripiprazole, AS01B, AS02B, AS02V, Azacitidine; Becatecarin, Bevacizumab, Bevirimat, Bortezomib, Bremelanotide; CAIV-T, Canfosfamide hydrochloride, CHR-2797, Ciclesonide, Clevidipine; Darbepoetin alfa, Decitabine, Degarelix acetate, Dendritic cell-based vaccine, Denosumab, Desloratadine, DMXB-Anabaseine, Duloxetine hydrochloride, Dutasteride; Ecogramostim, Eicosapentaenoic acid/docosahexaenoic acid, Eletriptan, Enzastaurin hydrochloride, Erlotinib hydrochloride, Escitalopram oxalate, Etoricoxib, Everolimus, Ezetimibe, Ezetimibe/simvastatin; Ferumoxytol, Fesoterodine fumarate, Fulvestrant; Gefitinib, GM-CSF DNA, GSK-690693; H5N1 avian flu vaccine, Hepatitis B hyperimmunoglobulin, Human Fibroblast Growth Factor 1, Hypericin-PVP; Icatibant acetate, Iclaprim, Immunoglobulin intravenous (human), Ipilimumab, ISS-1018; L19-IL-2, Lapuleucel-T, Laropiprant, Liposomal doxorubicin, LP-261, Lumiracoxib, LY-518674; MDV-3100, MGCD-0103, Mirabegron, MyoCell; NASHA/Dx, Niacin/laropiprant; O6-Benzylguanine, Ocrelizumab, Olmesartan medoxomil, Omalizumab; P-276-00, Paclitaxel nanoparticles, Paclitaxel nanoparticles, Padoporfin, Paliperidone, PAN-811, Pegaptanib octasodium, Pegfilgrastim, Pemetrexed disodium, PF-00299804, Pimecrolimus, Prasugrel, Pregabalin; Reolysin, Rimonabant, Rivaroxaban, Rosuvastatin calcium; Satraplatin, SCH-697243,Selenite sodium, Silodosin, Sorafenib, Sunitinib malate; Talarozole, Taxus, Temsirolimus, Tocilizumab, Tolevamer potassium sodium, Tremelimumab, TTP-889; Uracil; V-260, Valsartan/amlodipine besylate, Vardenafil hydrochloride hydrate, Varenicline tartrate, Varespladib, Vitespen, Voclosporin, VX-001; Xience V; Zotarolimus-eluting stent.

2.Gateways to clinical trials.
Tomillero A, Moral MA. Methods Find Exp Clin Pharmacol. 2009 Apr;31(3):183-226.
(+)-Dapoxetine hydrochloride, [(123)I]-BZA, 9-Aminocamptothecin; Abacavir sulfate/lamivudine, Adalimumab, Adefovir dipivoxil, Alemtuzumab, Alvocidib hydrochloride, Ambrisentan, Amsilarotene, Anacetrapib, Anakinra, Apricitabine, Aripiprazole, Arsenic trioxide, Atazanavir sulfate, Atazanavir/ritonavir, Atrasentan, Azacitidine; Banoxantrone, Bazedoxifene acetate, Bevacizumab, Bexarotene, Biphasic insulin aspart, Bortezomib, Bosentan, Bromfenac; Cachectin, Calcipotriol/betamethasone dipropionate, Canakinumab, Carfilzomib, CAT-354, CCX-282, Certolizumab pegol, Cetuximab, Choline fenofibrate, Clevudine, Clofarabine, CNTO-328, Corifollitropin alfa, Crofelemer; Daptomycin, Darbepoetin alfa, Darunavir, Dasatinib, Decitabine, Deferasirox, Denosumab, Duloxetine hydrochloride, Dutasteride; Emtricitabine, Enfuvirtide, Entecavir, Epoetin zeta, Erlotinib hydrochloride, Escitalopram oxalate, Eslicarbazepine acetate, Eszopiclone, Etravirine, Everolimus, Exenatide, Ezetimibe, Ezetimibe/simvastatin; Farglitazar, Febuxostat, Fosamprenavir calcium, FX-06; Gabapentin enacarbil, Gefitinib; HIVIS DNA; Imatinib mesylate, INCB- 18424, Indacaterol, Inotuzumab ozogamicin, Insulin detemir; JNJ-26854165; Lacosamide, Landiolol, Laromustine, Lenalidomide, Liposomal doxorubicin, L-NAME, Lopinavir, Lopinavir/ritonavir, Lumiracoxib; Maraviroc, Mepolizumab, Methoxy polyethylene glycol- epoetin-beta, Miglustat, MK-0493, MVA-CMDR, Mycophenolic acid sodium salt; Natalizumab, Nepafenac, Neratinib, Neridronic acid, Nesiritide, Nilotinib hydrochloride monohydrate; Olmesartan medoxomil, Omacetaxine mepesuccinate, Omalizumab; Paclitaxel poliglumex, Palifermin, Patupilone, Pegfilgrastim, Peginterferon alfa-2a, Peginterferon alfa-2b, Peginterferon alfa-2b/ ribavirin, Pemetrexed disodium, PHA-848125, Pitavastatin calcium, Posaconazole, Povidone-iodine liposome complex, Prasugrel, Pregabalin, Prucalopride; Raltegravir potassium, Retigabine, Revaprazan hydrochloride, rhFSH, Rilpivirine, Rivaroxaban, Romidepsin, Rosuvastatin calcium, RWJ-676070; SAR-109659, Sitagliptin phosphate monohydrate, Sorafenib, Stavudine/Lamivudine/Nevirapine, Sunitinib malate; Tadalafil, Telaprevir, Telbivudine, Tenofovir disoproxil fumarate, Tenofovir disoproxil fumarate/emtricitabine, Tenofovir disoproxil fumarate/emtricitabine/efavirenz, Teriparatide, Tigecycline, Tiotropium bromide, Tipifarnib, Tipranavir, Tocilizumab, Trifluridine/TPI; UP-780; Vandetanib, Vardenafil hydrochloride hydrate, Vatalanib succinate, Vitespen, Vorinostat; Yttrium 90 (90Y) ibritumomab tiuxetan; Zoledronic acid monohydrate.

3.The epidermal growth factor tyrosine kinase inhibitor AG1478 and erlotinib reverse ABCG2-mediated drug resistance.
Shi Z1, Parmar S, Peng XX, Shen T, Robey RW, Bates SE, Fu LW, Shao Y, Chen YM, Zang F, Chen ZS. Oncol Rep. 2009 Feb;21(2):483-9.
ABCG2 is an important member of ATP-binding cassette (ABC) transporter shown to confer drug resistance in cancer cells. Recent studies show that an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), gefitinib, is able to modulate the function of ABCG2 and reverse ABCG2-mediated multidrug resistance (MDR) in cancer cells. Additionally, ABCG2 expression has been shown to impact treatment efficacy and development of side-effects in patients receiving gefitinib. However, it is unclear whether other EGFR TKIs interact with ABCG2 in a similar manner. In the present study, we investigated the interaction of two other EGFR TKIs, AG1478 and erlotinib, with ABCG2. Our data show that AG1478 and erlotinib potently sensitized drug-resistant cells overexpressing either wild-type or mutated ABCG2 to the ABCG2 substrate anti-cancer drugs flavopiridol and mitoxantrone. Neither AG1478 nor erlotinib sensitized ABCG2-overexpressing cells to drugs that are not substrates of ABCG2 nor did they impact drug sensitivity of parental cells.

4.Gateways to clinical trials.
Tomillero A, Moral MA. Methods Find Exp Clin Pharmacol. 2009 May;31(4):263-98.
(-)-Gossypol; Abacavir sulfate/lamivudine, ACAM-1000, ACE-011, Agomelatine, AGS-004, Alemtuzumab, Alvocidib hydrochloride, AMG-317, Amlodipine, Aripiprazole, Atazanavir sulfate, Azacitidine; Becatecarin, Belinostat, Bevacizumab, BMS-387032, BMS-690514, Bortezomib; Casopitant mesylate, Cetuximab, Choline fenofibrate, CK-1827452, Clofarabine, Conivaptan hydrochloride; Dabigatran etexilate, DADMe-Immucillin-H, Darbepoetin alfa, Darunavir, Dasatinib, DC-WT1, Decitabine, Deferasirox, Degarelix acetate, Denenicokin, Denosumab, Dienogest, Duloxetine hydrochloride; Ecogramostim, Eculizumab, Edoxaban tosilate, Elacytarabine, Elesclomol, Eltrombopag olamine, Enfuvirtide, Enzastaurin hydrochloride, Eribulin mesilate, Erlotinib hydrochloride, Escitalopram oxalate, Eszopiclone, Etravirine; Flibanserin, Fludarabine, Fondaparinux sodium, Fosamprenavir calcium; Gefitinib, Genistein; I-131-L19-SIP, Idrabiotaparinux sodium, Imatinib mesylate, IMGN-901, Ipilimumab; Laromustine, Lenalidomide, Liposomal cisplatin, Liraglutide, Lisdexamfetamine mesilate, Lopinavir, Lopinavir/ritonavir; Maraviroc, MDV-3100, Mecasermin rinfabate, MP-470, Mycophenolic acid sodium salt; Naproxcinod, NB-002, Nesiritide, Nilotinib hydrochloride monohydrate, NK-012; Palonosetron hydrochloride, Panobinostat, Pegfilgrastim, Peginterferon alfa-2a, Pitavastatin calcium, PL-3994, Plerixafor hydrochloride, Plitidepsin, PM-10450; Raltegravir potassium, Recombinant human soluble thrombomodulin, ReoT3D, RHAMM R3 peptide, Rivaroxaban, Romiplostim, Rosuvastatin calcium, Rozrolimupab; Sabarubicin hydrochloride, Salinosporamide A, Sirolimus-eluting stent, Smallpox (Vaccinia) Vaccine, Live, Sorafenib; Tenofovir disoproxil fumarate, Tenofovir disoproxil fumarate/emtricitabine, Teriparatide, Tipifarnib, Tipranavir, Trabectedin, Trifluridine/TPI; Vardenafil hydrochloride hydrate, Vinflunine, Volociximab, Vorinostat; Ximelagatran; Yttrium 90 (90Y) ibritumomab tiuxetan; Ziprasidone hydrochloride, Zoledronic acid monohydrate.

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